PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 2616041-1 1989 The inhibitory effects of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on monoamine oxidase (MAO; EC 1.4.3.4) enzyme activities in human hippocampal and rat striatal homogenates have been studied. tha 62-65 monoamine oxidase A Rattus norvegicus 70-87 2616041-1 1989 The inhibitory effects of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on monoamine oxidase (MAO; EC 1.4.3.4) enzyme activities in human hippocampal and rat striatal homogenates have been studied. tha 62-65 monoamine oxidase A Rattus norvegicus 89-92 2616041-2 1989 The activities of MAO-A and MAO-B were estimated radiochemically, in-vitro, in human hippocampus and rat striatum in the presence of various concentrations of THA with [2-14C]hydroxytryptamine binoxalate (100 microM) and beta-[ethyl-14C]phenylethylamine hydrochloride (20 microM) as substrates for the respective enzyme form. tha 159-162 monoamine oxidase A Homo sapiens 18-23 2616041-2 1989 The activities of MAO-A and MAO-B were estimated radiochemically, in-vitro, in human hippocampus and rat striatum in the presence of various concentrations of THA with [2-14C]hydroxytryptamine binoxalate (100 microM) and beta-[ethyl-14C]phenylethylamine hydrochloride (20 microM) as substrates for the respective enzyme form. tha 159-162 monoamine oxidase B Homo sapiens 28-33 2616041-3 1989 THA was found to inhibit both MAO-A and MAO-B activities reversibly and competitively, with inhibition constants (Ki) of 12.5 microM and greater than 500 microM respectively, of the rat striatal enzymes. tha 0-3 monoamine oxidase A Rattus norvegicus 30-35 2616041-3 1989 THA was found to inhibit both MAO-A and MAO-B activities reversibly and competitively, with inhibition constants (Ki) of 12.5 microM and greater than 500 microM respectively, of the rat striatal enzymes. tha 0-3 monoamine oxidase B Rattus norvegicus 40-45 2616041-4 1989 From this it can be extrapolated that at therapeutic tissue concentrations of THA (10(-8) to 10(-6) M), more than 20% of the MAO-A activity should be inhibited. tha 78-81 monoamine oxidase A Rattus norvegicus 125-130 2616041-5 1989 Thus it is possible that inhibition of MAO may be involved in the therapeutic action of THA in Alzheimer"s disease. tha 88-91 monoamine oxidase A Rattus norvegicus 39-42 2611486-1 1989 1 Tetrahydroaminoacridine (THA) is an acetylcholinesterase (AChE) inhibitor which may have a greater therapeutic effect in Alzheimer-type dementia (ATD) than other cholinergic agents. tha 2-25 acetylcholinesterase Rattus norvegicus 38-58 2611486-1 1989 1 Tetrahydroaminoacridine (THA) is an acetylcholinesterase (AChE) inhibitor which may have a greater therapeutic effect in Alzheimer-type dementia (ATD) than other cholinergic agents. tha 2-25 acetylcholinesterase Rattus norvegicus 60-64 2611486-1 1989 1 Tetrahydroaminoacridine (THA) is an acetylcholinesterase (AChE) inhibitor which may have a greater therapeutic effect in Alzheimer-type dementia (ATD) than other cholinergic agents. tha 27-30 acetylcholinesterase Rattus norvegicus 38-58 2611486-1 1989 1 Tetrahydroaminoacridine (THA) is an acetylcholinesterase (AChE) inhibitor which may have a greater therapeutic effect in Alzheimer-type dementia (ATD) than other cholinergic agents. tha 27-30 acetylcholinesterase Rattus norvegicus 60-64 2606156-3 1989 In vitro, THA inhibits acetylcholinesterase (AChE) (IC50 = 223 nM) and blocks [3H]AFDX-116 (M2) and [3H]telenzepine (M1) binding (IC50 s of 1.5 and 9.1 microM respectively). tha 10-13 acetylcholinesterase Rattus norvegicus 45-49 2606156-9 1989 We conclude that brain AChE inhibition by THA is sufficient to explain its purported therapeutic activity in Alzheimer"s disease and that its favorable brain/plasma distribution in vivo may account for its central cholinergic action without inducing the severe peripheral cholinergic effects typically seen with other AChE inhibitors. tha 42-45 acetylcholinesterase Rattus norvegicus 23-27 2594683-6 1989 Although the inhibition of acetylcholinesterase by tacrine is well documented, regional uptake in brain did not correlate consistently with distribution of the enzyme, supporting suggestions by others that the alleged action of tacrine in treatment of senile dementia may be by mechanisms other than cholinesterase inhibition. tha 51-58 acetylcholinesterase Rattus norvegicus 27-47 33892271-3 2021 Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), is ensured via a "foot-in-the-door" open-channel blockage, and that interestingly both tacrine and 7-MEOTA are slightly more potent at the GluN1/GluN2A receptors when compared with the GluN1/GluN2B receptors. tha 62-69 glutamate ionotropic receptor NMDA type subunit 2B Homo sapiens 309-315 2760841-1 1989 Tetrahydroaminoacridine (THA) is known to be a potent centrally acting cholinesterase inhibitor. tha 0-23 butyrylcholinesterase Rattus norvegicus 71-85 2760841-1 1989 Tetrahydroaminoacridine (THA) is known to be a potent centrally acting cholinesterase inhibitor. tha 25-28 butyrylcholinesterase Rattus norvegicus 71-85 2913485-1 1989 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine) showed an apparent noncompetitive inhibition of Torpedo acetylcholinesterase (AChE) with a dissociation constant, Ki, of 8.5 nM. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-121 2913485-1 1989 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine) showed an apparent noncompetitive inhibition of Torpedo acetylcholinesterase (AChE) with a dissociation constant, Ki, of 8.5 nM. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 123-127 2913485-1 1989 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine) showed an apparent noncompetitive inhibition of Torpedo acetylcholinesterase (AChE) with a dissociation constant, Ki, of 8.5 nM. tha 9-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-121 2913485-1 1989 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine) showed an apparent noncompetitive inhibition of Torpedo acetylcholinesterase (AChE) with a dissociation constant, Ki, of 8.5 nM. tha 9-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 123-127 2913485-3 1989 An extrinsic CD band was induced at 348 nm, with a molar ellipticity of 35,000 deg cm2 dmol-1 (bases on tacrine), when each AChE subunit (Mr = 67,000) was saturated with one tacrine (mol/mol). tha 104-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-128 2913485-3 1989 An extrinsic CD band was induced at 348 nm, with a molar ellipticity of 35,000 deg cm2 dmol-1 (bases on tacrine), when each AChE subunit (Mr = 67,000) was saturated with one tacrine (mol/mol). tha 174-181 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-128 2913485-4 1989 With this band as a probe, the bound tacrine could be displaced by edrophonium or decamethonium, both of which are known to bind to the anionic site at the active center of AChE, but not by propidium, which binds to the peripheral site of the enzyme. tha 37-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 173-177 2913485-5 1989 Tacrine protected AChE from inactivation by diisopropylfluorophosphate (DFP). tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 18-22 2913485-6 1989 AChE completely lost its enzymatic activity when 1 mol of DFP was bound per mol of subunit upon incubation of 7 microM AChE (subunit) with 100 microM DFP for 40 min, but tacrine-treated AChE retained 60% of its activity and bound only 0.2 mol of DFP per mol of subunit under similar conditions. tha 170-177 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 2913485-7 1989 The corresponding CD, at 348 nm, of the AChE-tacrine-DFP complex increased or decreased gradually, depending on the order of addition of tacrine and DFP, and reached an equilibrium value (80% of its original) after 2 days. tha 45-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-44 2913485-8 1989 The difference absorption spectrum of the AChE-tacrine-DFP complex was the same as that of the AChE-tacrine complex. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 2913485-8 1989 The difference absorption spectrum of the AChE-tacrine-DFP complex was the same as that of the AChE-tacrine complex. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 2913485-8 1989 The difference absorption spectrum of the AChE-tacrine-DFP complex was the same as that of the AChE-tacrine complex. tha 100-107 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 2913485-8 1989 The difference absorption spectrum of the AChE-tacrine-DFP complex was the same as that of the AChE-tacrine complex. tha 100-107 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 2602408-1 1989 Despite a strong rationale for the use of cholinesterase (ChE) inhibitors and related drugs to augment cholinergic function as palliative treatment for Alzheimer dementia, this approach met with limited and variable success until the striking results recently reported with tacrine (THA). tha 274-281 butyrylcholinesterase Rattus norvegicus 58-61 2602408-1 1989 Despite a strong rationale for the use of cholinesterase (ChE) inhibitors and related drugs to augment cholinergic function as palliative treatment for Alzheimer dementia, this approach met with limited and variable success until the striking results recently reported with tacrine (THA). tha 283-286 butyrylcholinesterase Rattus norvegicus 58-61 2602408-4 1989 Consistent with previous reports, we find an in vitro IC50 of 1 microM THA or less for brain or red blood cell AChE, dependent on the substrate concentration. tha 71-74 acetylcholinesterase Rattus norvegicus 111-115 2602408-6 1989 However, after in vivo THA, the inhibition of plasma ChE or brain AChE declined as a log function of tissue dilution. tha 23-26 butyrylcholinesterase Rattus norvegicus 53-56 2602408-6 1989 However, after in vivo THA, the inhibition of plasma ChE or brain AChE declined as a log function of tissue dilution. tha 23-26 acetylcholinesterase Rattus norvegicus 66-70 2602408-9 1989 Pons-medulla AChE was much less sensitive to the effects of THA than hippocampus, cortex, cerebellum or plasma ChE, particularly at doses of 2.5 mg/kg or less. tha 60-63 acetylcholinesterase Rattus norvegicus 13-17 2602408-9 1989 Pons-medulla AChE was much less sensitive to the effects of THA than hippocampus, cortex, cerebellum or plasma ChE, particularly at doses of 2.5 mg/kg or less. tha 60-63 butyrylcholinesterase Rattus norvegicus 14-17 2602408-10 1989 In these other brain regions, AChE was inhibited 22-44% after doses of 1.25 to 2.5 mg/kg THA, the dose range which maximally improved retention performance in mice. tha 89-92 acetylcholinesterase Mus musculus 30-34 3185960-3 1988 IC50 values (the concentration required to reduce enzyme activity by 50%) for the inhibition of total tissue AChE were 7.9 x 10(-7) M and 4.5 x 10(-8) M for THA and physostigmine, respectively, and similar values were also obtained for individual molecular forms of AChE (monomer G1, dimer G2 and tetramer G4) separated by sucrose density gradient centrifugation. tha 157-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 109-113 3435078-1 1987 The histochemical distribution of cholinesterases in the cerebral cortex and their response to cholinesterase inhibitors such as physostigmine and tetrahydroaminoacridine (THA) were investigated in brains from patients with Alzheimer"s disease and control subjects. tha 147-170 butyrylcholinesterase Homo sapiens 34-48 3435078-1 1987 The histochemical distribution of cholinesterases in the cerebral cortex and their response to cholinesterase inhibitors such as physostigmine and tetrahydroaminoacridine (THA) were investigated in brains from patients with Alzheimer"s disease and control subjects. tha 172-175 butyrylcholinesterase Homo sapiens 34-48 3435078-3 1987 In keeping with their well-known cholinomimetic effects, physostigmine and THA effectively inhibited this cholinesterase activity. tha 75-78 butyrylcholinesterase Homo sapiens 106-120 7028622-8 1981 We postulate that this vasodilator system might play a role in the maintenance of normotension in pregnancy, counteracting tha effect of the renin-angiotensin-aldosterone system. tha 13-16 renin Homo sapiens 141-146 155828-1 1979 In vivo inhibition of blood acetylcholinesterase activity by 9-amino-1, 2, 3, 4-tetrahydroacridine, its 7-methoxy derivative and physostigmine was studied in rats. tha 61-98 acetylcholinesterase Rattus norvegicus 28-48 1236951-1 1975 The dissociation constants have been determined and compared for a series of reversible, noncovalent inhibitors of eel acetylcholinesterase that are structurally related to the very potent inhibitor, 1,2,3,4-tetrahydro-9-aminoacridine (THA). tha 200-234 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-139 1236951-1 1975 The dissociation constants have been determined and compared for a series of reversible, noncovalent inhibitors of eel acetylcholinesterase that are structurally related to the very potent inhibitor, 1,2,3,4-tetrahydro-9-aminoacridine (THA). tha 236-239 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-139 1191768-1 1975 The capacity of reversible inhibitors--galanthamine and tacrine--to protect the cholinesterase of rat and mouse brain from the thermal denaturation with the action of the temperature of 56 and 58 degrees C was revealed. tha 56-63 butyrylcholinesterase Rattus norvegicus 80-94 2616041-0 1989 Tetrahydroaminoacridine inhibits human and rat brain monoamine oxidase. tha 0-23 monoamine oxidase A Rattus norvegicus 53-70 2616041-1 1989 The inhibitory effects of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on monoamine oxidase (MAO; EC 1.4.3.4) enzyme activities in human hippocampal and rat striatal homogenates have been studied. tha 26-60 monoamine oxidase A Rattus norvegicus 70-87 2616041-1 1989 The inhibitory effects of 1,2,3,4-tetrahydro-9-aminoacridine (THA) on monoamine oxidase (MAO; EC 1.4.3.4) enzyme activities in human hippocampal and rat striatal homogenates have been studied. tha 26-60 monoamine oxidase A Rattus norvegicus 89-92 2789791-0 1989 Estimation of plasma tacrine concentrations using an in vitro cholinesterase inhibition assay. tha 21-28 butyrylcholinesterase Homo sapiens 62-76 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 0-3 butyrylcholinesterase Homo sapiens 81-95 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 0-3 butyrylcholinesterase Homo sapiens 97-100 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 5-40 butyrylcholinesterase Homo sapiens 81-95 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 5-40 butyrylcholinesterase Homo sapiens 97-100 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 42-49 butyrylcholinesterase Homo sapiens 81-95 2789791-1 1989 THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. tha 42-49 butyrylcholinesterase Homo sapiens 97-100 2804555-12 1989 In vitro THA was a potent non-competitive inhibitor of rat brain cholinesterase (IC50: 57 +/- 6 nM) and bovine erythrocyte acetylcholinesterase (IC50: 50 +/- 10 nM) but was a more potent inhibitor of horse serum butyrylcholinesterase (IC50: 7.2 +/- 1.4 nM). tha 9-12 butyrylcholinesterase Rattus norvegicus 65-79 2804555-17 1989 It is concluded that THA is a reversible non-competitive inhibitor of cholinesterase with a long half life (compared with physostigmine). tha 21-24 butyrylcholinesterase Rattus norvegicus 70-84 2761772-0 1989 Tacrine slows the rate of ageing of sarin-inhibited acetylcholinesterase. tha 0-7 acetylcholinesterase Rattus norvegicus 52-72 2721578-1 1989 The actions of 9-amino-1,2,3,4-tetrahydroacridine (THA) were studied on rat CA1 pyramidal neurones under voltage-clamp in transverse slices of hippocampus maintained in vitro. tha 51-54 carbonic anhydrase 1 Rattus norvegicus 76-79 2721578-3 1989 More sensitive to the action of THA was the outward K+ current activated in CA1 neurones by 5-HT, adenosine and baclofen. tha 32-35 carbonic anhydrase 1 Rattus norvegicus 76-79 2655861-3 1989 Tetrahydroaminoacridine (THA), an acetylcholinesterase inhibitor, is currently being investigated at the McGill Centre for Studies in Aging. tha 0-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-54 2655861-3 1989 Tetrahydroaminoacridine (THA), an acetylcholinesterase inhibitor, is currently being investigated at the McGill Centre for Studies in Aging. tha 25-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-54 2893967-5 1988 In addition the affinity of THA for alpha-1, alpha-2 and beta-adrenoceptors, for D-2 dopamine, S-1a and S-2 serotonin and for muscarinic receptors was investigated. tha 28-31 BCL2 related protein A1 Homo sapiens 36-43 2893967-5 1988 In addition the affinity of THA for alpha-1, alpha-2 and beta-adrenoceptors, for D-2 dopamine, S-1a and S-2 serotonin and for muscarinic receptors was investigated. tha 28-31 glycoprotein hormone subunit alpha 2 Homo sapiens 45-52 3103482-3 1986 Using C18 Bond Elut columns and an HPLC/fluorometry system, this assay exhibits a considerable improvement in sensitivity over previous uv methods, and allows routine testing of THA levels in serum samples of reasonable volume from human subjects. tha 178-181 Bardet-Biedl syndrome 9 Homo sapiens 6-9 33979725-3 2021 The steady-state emission spectrum results showed that presence of static quenching mode for piperine, tacrine, curcumin, silibinin molecules with BSA and AChE complexes separately and this excitation-emission matrix analysis suggest that formation of ground-state complex between piperine, tacrine, curcumin, silibinin drugs and both BSA, AChE protein molecules. tha 103-110 acetylcholinesterase (Cartwright blood group) Homo sapiens 155-159 33979725-3 2021 The steady-state emission spectrum results showed that presence of static quenching mode for piperine, tacrine, curcumin, silibinin molecules with BSA and AChE complexes separately and this excitation-emission matrix analysis suggest that formation of ground-state complex between piperine, tacrine, curcumin, silibinin drugs and both BSA, AChE protein molecules. tha 291-298 acetylcholinesterase (Cartwright blood group) Homo sapiens 155-159 33892271-3 2021 Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), is ensured via a "foot-in-the-door" open-channel blockage, and that interestingly both tacrine and 7-MEOTA are slightly more potent at the GluN1/GluN2A receptors when compared with the GluN1/GluN2B receptors. tha 62-69 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 257-262 33892271-3 2021 Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), is ensured via a "foot-in-the-door" open-channel blockage, and that interestingly both tacrine and 7-MEOTA are slightly more potent at the GluN1/GluN2A receptors when compared with the GluN1/GluN2B receptors. tha 62-69 glutamate ionotropic receptor NMDA type subunit 2A Homo sapiens 263-269 33892271-3 2021 Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), is ensured via a "foot-in-the-door" open-channel blockage, and that interestingly both tacrine and 7-MEOTA are slightly more potent at the GluN1/GluN2A receptors when compared with the GluN1/GluN2B receptors. tha 62-69 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 303-308 33829779-4 2021 We applied a framework combination of functionalized CNSL components and well-established acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) tacrine templates. tha 147-154 butyrylcholinesterase Mus musculus 141-145 33539054-2 2021 BACKGROUND: One goal of THA is to restore the anatomic hip center, which can be achieved in hips with developmental dysplasia by placing cups at the level of the native acetabulum. tha 24-27 hedgehog interacting protein Homo sapiens 55-58 34024109-0 2021 Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer"s Disease. tha 19-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 34024109-0 2021 Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer"s Disease. tha 19-26 glycogen synthase kinase 3 beta Mus musculus 66-71 33930191-0 2021 Promising tacrine/huperzine A- based dimeric AChE inhibitors for neurodegenerative disorders: from relieving symptoms to modifying diseases through multi-target. tha 10-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-49 33887253-4 2021 The cholinesterase inhibitor, tacrine, was used as a comparator. tha 30-37 butyrylcholinesterase Rattus norvegicus 4-18 33839958-6 2021 Furthermore, because of the inhibition effect of tacrine on AChE, tacrine is also detected through the colorimetric AChE assay system within the concentrations range 0.025-0.4 muM with a LOD of 0.00229 muM. tha 49-56 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 33839958-6 2021 Furthermore, because of the inhibition effect of tacrine on AChE, tacrine is also detected through the colorimetric AChE assay system within the concentrations range 0.025-0.4 muM with a LOD of 0.00229 muM. tha 66-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 33839958-6 2021 Furthermore, because of the inhibition effect of tacrine on AChE, tacrine is also detected through the colorimetric AChE assay system within the concentrations range 0.025-0.4 muM with a LOD of 0.00229 muM. tha 66-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 33844597-3 2021 AChE inhibitors can have therapeutic applications (e.g., tacrine and donepezil) or neurotoxic consequences (e.g., insecticides and nerve agents). tha 57-64 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 33869976-1 2021 A new series of N-aryltacrine derivatives were designed and synthesized as cholinesterase inhibitors by the late-stage modification of tacrine, using the palladium-catalyzed Buchwald-Hartwig cross-coupling reaction. tha 22-29 butyrylcholinesterase Homo sapiens 75-89 33503372-7 2021 Moreover, its excellent work for inhibition efficacy elucidation was also proved with the accuracy IC50 of tacrine for BChE (8.6 nM), giving rise to an expanded application for trace pesticide determination. tha 107-114 butyrylcholinesterase Homo sapiens 119-123 33645607-0 2021 Tacrine-sugar mimetic conjugates as enhanced cholinesterase inhibitors. tha 0-7 butyrylcholinesterase Homo sapiens 45-59 33645607-3 2021 Two of the heterodimers were significantly stronger acetylcholinesterase inhibitors than the monomeric tacrine. tha 103-110 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 33189440-4 2021 Herein, we report a series of ROS-responsive prodrugs based on multi-target-directed ligands (MTDLs) approach, which can specifically release tacrine derivatives and ibuprofen under oxidation of ROS and show acetylcholinesterase (AChE)-inhibiting, neuron-protective and anti-inflammatory effects in extracellular or intracellular assays. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 208-228 33517001-0 2021 7-Amine-spiro[chromeno[4,3-b]quinoline-6,1"-cycloalkanes]: Synthesis and cholinesterase inhibitory activity of structurally modified tacrines. tha 133-141 butyrylcholinesterase Homo sapiens 73-87 33672694-2 2021 The ability of human topoisomerase I (hTOPI) and II to relax supercoiled plasmid DNA in the presence of various concentrations of the tacrine-coumarin hybrid molecules was studied with agarose gel electrophoresis. tha 134-141 DNA topoisomerase I Homo sapiens 38-43 33189440-4 2021 Herein, we report a series of ROS-responsive prodrugs based on multi-target-directed ligands (MTDLs) approach, which can specifically release tacrine derivatives and ibuprofen under oxidation of ROS and show acetylcholinesterase (AChE)-inhibiting, neuron-protective and anti-inflammatory effects in extracellular or intracellular assays. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 230-234 33583371-5 2021 By using tacrine to target the catalytic active site (CAS), the tacrine-based MTDLs can act on both CAS and peripheral anion site (PAS) of AChE so as to serve as a dual-site AChE inhibitor. tha 9-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 33583371-5 2021 By using tacrine to target the catalytic active site (CAS), the tacrine-based MTDLs can act on both CAS and peripheral anion site (PAS) of AChE so as to serve as a dual-site AChE inhibitor. tha 9-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 33583371-5 2021 By using tacrine to target the catalytic active site (CAS), the tacrine-based MTDLs can act on both CAS and peripheral anion site (PAS) of AChE so as to serve as a dual-site AChE inhibitor. tha 64-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 33583371-5 2021 By using tacrine to target the catalytic active site (CAS), the tacrine-based MTDLs can act on both CAS and peripheral anion site (PAS) of AChE so as to serve as a dual-site AChE inhibitor. tha 64-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 33338868-0 2021 Conjugation of tacrine with genipin derivative not only enhances effects on AChE but also leads to autophagy against Alzheimer"s disease. tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-80 33338868-2 2021 Compound 8-7 was confirmed as the most active AChE inhibitor with IC50 value of 5.8 +- 1.4 nM, which was 7.72-fold stronger than tacrine. tha 129-136 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 33540879-6 2021 Dual-drug combinations of berberine and tacrine (BerTac), berberine and galantamine (BerGal), and tacrine and donepezil (TacDon) all produced synergistic outcomes for AChE inhibition. tha 98-105 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-171 33583371-4 2021 Tacrine, as the first acetylcholinesterase (AChE) inhibitor, has been discontinued because of its hepatotoxicity, but its core structure is simple and easy to modify. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-48 33448662-0 2021 Multi-Targeting Tacrine Conjugates with Cholinesterase and Amyloid-Beta Inhibitory Activities: New Anti-Alzheimer"s Agents. tha 16-23 butyrylcholinesterase Homo sapiens 40-54 33448662-0 2021 Multi-Targeting Tacrine Conjugates with Cholinesterase and Amyloid-Beta Inhibitory Activities: New Anti-Alzheimer"s Agents. tha 16-23 amyloid beta precursor protein Homo sapiens 59-71 33191671-5 2021 In this work, RGD adhesion peptides and an antivascular endothelial growth factor receptor-2 (VEGF-R2) DNA aptamer are incorporated into a tHA-PEGDA hydrogel to make a bifunctional hyaluronic acid hydrogel. tha 139-142 kinase insert domain receptor Homo sapiens 94-101 33421953-1 2021 A series of tacrine - benzothiazole hybrids incorporate inhibitors of acetylcholinesterase (AChE), amyloid beta (Abeta) aggregation and mitochondrial enzyme ABAD, whose interaction with Abeta leads to mitochondrial dysfunction, into a single molecule. tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-90 33421953-1 2021 A series of tacrine - benzothiazole hybrids incorporate inhibitors of acetylcholinesterase (AChE), amyloid beta (Abeta) aggregation and mitochondrial enzyme ABAD, whose interaction with Abeta leads to mitochondrial dysfunction, into a single molecule. tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 33421953-1 2021 A series of tacrine - benzothiazole hybrids incorporate inhibitors of acetylcholinesterase (AChE), amyloid beta (Abeta) aggregation and mitochondrial enzyme ABAD, whose interaction with Abeta leads to mitochondrial dysfunction, into a single molecule. tha 12-19 amyloid beta precursor protein Homo sapiens 113-118 33076048-6 2021 This biosensor obtained a good linear range from 0.02 to 1 mU/mL and an extremely low detection limit of 15 muU/mL for AChE assay, as well as a sensitive screening for tacrine and an excellent applicability in human serum samples. tha 168-175 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 33169934-3 2021 Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 19-33 33397254-2 2021 CYP1A2 metabolises many clinical drugs, such as phenacetin, caffeine, clozapine, tacrine, propranolol, and mexiletine. tha 81-88 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 0-6 33076048-4 2021 Owing to the inhibiting effect of tacrine to the AChE activity, the decomposition of MnO2 was hindered, thus leading to the fluorescence recovery. tha 34-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 49-53 33383645-7 2020 In turn, BBB-permeability studies were inconclusive, and conjugation to the CPP led to a considerable loss of Tacrine function as an AChE inhibitor. tha 110-117 acetylcholinesterase (Cartwright blood group) Homo sapiens 133-137 33216529-0 2020 Novel Multitarget Directed Tacrine Hybrids as Anti-Alzheimer"s Compounds Improved Synaptic Plasticity and Cognitive Impairment in APP/PS1 Transgenic Mice. tha 27-34 presenilin 1 Mus musculus 134-137 33216529-3 2020 In this study, a novel multitarget derivative based on tacrine (named 9i), which could work simultaneously on more than one pathological target, was used to treat AD model APP/PS1 transgenic mice. tha 55-62 presenilin 1 Mus musculus 176-179 33299418-9 2020 The ALP activity test revealed that groups exposed to THA for 7, 11, and 15 days showed higher ALP activity than the control groups (p < 0.05). tha 54-57 alkaline phosphatase, placental Homo sapiens 4-7 33308120-5 2022 This manuscript describes the new tacrine derivatives tethered to isatin Schiff bases through alkanoyl linker and screened for cholinesterase inhibitory activity. tha 34-41 butyrylcholinesterase Homo sapiens 127-141 33153323-2 2020 The measurement of gas-phase basicity (GB) and proton affinity (PA) values of four important and commercially available drugs for Alzheimer"s disease namely, rivastigmine, galantamine, memantine, and tacrine, is attempted for the first time. tha 200-207 galactosamine (N-acetyl)-6-sulfatase Homo sapiens 19-22 33299418-9 2020 The ALP activity test revealed that groups exposed to THA for 7, 11, and 15 days showed higher ALP activity than the control groups (p < 0.05). tha 54-57 alkaline phosphatase, placental Homo sapiens 95-98 33282174-6 2020 Tartrate resistant acid phosphatase (TRAP) staining showed high osteoclast activity along with osteogenesis, especially in PU/THA and PU/Ag-THA groups. tha 126-129 acid phosphatase 5, tartrate resistant Rattus norvegicus 0-35 33282174-6 2020 Tartrate resistant acid phosphatase (TRAP) staining showed high osteoclast activity along with osteogenesis, especially in PU/THA and PU/Ag-THA groups. tha 126-129 acid phosphatase 5, tartrate resistant Rattus norvegicus 37-41 33282174-6 2020 Tartrate resistant acid phosphatase (TRAP) staining showed high osteoclast activity along with osteogenesis, especially in PU/THA and PU/Ag-THA groups. tha 140-143 acid phosphatase 5, tartrate resistant Rattus norvegicus 0-35 33282174-6 2020 Tartrate resistant acid phosphatase (TRAP) staining showed high osteoclast activity along with osteogenesis, especially in PU/THA and PU/Ag-THA groups. tha 140-143 acid phosphatase 5, tartrate resistant Rattus norvegicus 37-41 33047663-1 2022 Recently, we designed and synthesized a subnanomolar, reversible, dual-binding site acetylcholinesterase (AChE) inhibitor which consists of the tacrine and aroylacrylic acid phenylamide moieties, mutually linked by eight methylene units. tha 144-151 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-104 33047663-1 2022 Recently, we designed and synthesized a subnanomolar, reversible, dual-binding site acetylcholinesterase (AChE) inhibitor which consists of the tacrine and aroylacrylic acid phenylamide moieties, mutually linked by eight methylene units. tha 144-151 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 33299418-10 2020 It is concluded that THA had no cytotoxic effect on pulp cells; furthermore, it enhanced proliferation as well as ALP activity of the pulp cells. tha 21-24 alkaline phosphatase, placental Homo sapiens 114-117 32155891-0 2020 A Second Look at the Crystal Structures of Drosophila melanogaster Acetylcholinesterase in Complex with Tacrine Derivatives Provides Insights Concerning Catalytic Intermediates and the Design of Specific Insecticides. tha 104-111 Acetylcholine esterase Drosophila melanogaster 67-87 33195011-0 2020 Molecular Dynamics Revealing a Detour-Forward Release Mechanism of Tacrine: Implication for the Specific Binding Characteristics in Butyrylcholinesterase. tha 67-74 butyrylcholinesterase Homo sapiens 132-153 33195011-2 2020 Here, all-atom molecular dynamics simulations of butyrylcholinesterase with tacrine complex were designed to characterize inhibitor binding modes, strengths, and the hydrogen-bond dependent non-covalent release mechanism. tha 76-83 butyrylcholinesterase Homo sapiens 49-70 33195011-6 2020 The residues including Asp70, Ser79, Trp82, Gly116, Thr120, Tyr332, and His438 were identified to play major roles in the stabilization of tacrine in the pocket of BChE, where hydrogen bonding and pi-pi interactions are significant factors. tha 139-146 butyrylcholinesterase Homo sapiens 164-168 32825138-0 2020 Merged Tacrine-Based, Multitarget-Directed Acetylcholinesterase Inhibitors 2015-Present: Synthesis and Biological Activity. tha 7-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 43-63 32825138-3 2020 Tacrine, the first acetylcholinesterase inhibitor used clinically but withdrawn due to hepatotoxicity concerns, remains an important starting point in research for the development of multitarget-directed acetylcholinesterase inhibitors. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-39 32825138-3 2020 Tacrine, the first acetylcholinesterase inhibitor used clinically but withdrawn due to hepatotoxicity concerns, remains an important starting point in research for the development of multitarget-directed acetylcholinesterase inhibitors. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 204-224 32825138-4 2020 This review highlights tacrine-based, multitarget-directed acetylcholinesterase inhibitors published in the literature since 2015 with a specific focus on merged compounds (i.e., compounds where tacrine and a second pharmacophore show significant overlap in structure). tha 23-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-79 32453420-8 2020 Finally, we identified tacrine hydrochloride as a potential drug to inhibit aberrant CLK3-induced CCA. tha 23-44 CDC like kinase 3 Homo sapiens 85-89 31847645-0 2020 Tacrine modulates Kv2.1 channel gene expression and cell proliferation. tha 0-7 potassium voltage-gated channel subfamily B member 1 Homo sapiens 18-23 31847645-1 2020 Besides as a cholinesterase (ChE) inhibitor, tacrine is able to act on multiple targets such as nicotinic receptors (nAChRs) and voltage-gated K+ (Kv) channels. tha 45-52 butyrylcholinesterase Homo sapiens 13-27 31847645-1 2020 Besides as a cholinesterase (ChE) inhibitor, tacrine is able to act on multiple targets such as nicotinic receptors (nAChRs) and voltage-gated K+ (Kv) channels. tha 45-52 butyrylcholinesterase Homo sapiens 29-32 31847645-3 2020 Nevertheless, limited data are available concerning the relationship between tacrine and Kv2.1 channels. tha 77-84 potassium voltage-gated channel subfamily B member 1 Homo sapiens 89-94 31847645-4 2020 In the present study, incubation with tacrine induced a significant reduction of the mRNA level of Kv2.1 channels heterologously expressed in HEK293 cells. tha 38-45 potassium voltage-gated channel subfamily B member 1 Homo sapiens 99-104 31847645-6 2020 Moreover, the proliferation rates of HEK293 cells with Kv2.1 channel were substantially enhanced after treatment with this chemical for 24 h. Similar results were also detected after exposure to tacrine in N2A cells with native expression of Kv2.1 channels. tha 195-202 potassium voltage-gated channel subfamily B member 1 Homo sapiens 55-60 31847645-6 2020 Moreover, the proliferation rates of HEK293 cells with Kv2.1 channel were substantially enhanced after treatment with this chemical for 24 h. Similar results were also detected after exposure to tacrine in N2A cells with native expression of Kv2.1 channels. tha 195-202 potassium voltage gated channel, Shab-related subfamily, member 1 Mus musculus 242-247 31847645-7 2020 These lines of evidence indicate that application of tacrine downregulates the expression of Kv2.1 channels and increase cell proliferation. tha 53-60 potassium voltage-gated channel subfamily B member 1 Homo sapiens 93-98 31847645-8 2020 The effect of tacrine on Kv2.1 channels may provide an alternative explanation for its neuroprotective action. tha 14-21 potassium voltage-gated channel subfamily B member 1 Homo sapiens 25-30 32473192-0 2020 Tacrine accelerates spatial long-term memory via improving impaired neural oscillations and modulating GAD isomers including neuro-receptors in the hippocampus of APP/PS1 AD mice. tha 0-7 presenilin 1 Mus musculus 167-170 32473192-8 2020 Besides, the data represented that tacrine accelerated the expression of NR2B, SYP and GAD65 while it caused deceleration on the expression of GAD67 neurotransmitter and Abeta. tha 35-42 glutamate receptor, ionotropic, NMDA2B (epsilon 2) Mus musculus 73-77 32473192-8 2020 Besides, the data represented that tacrine accelerated the expression of NR2B, SYP and GAD65 while it caused deceleration on the expression of GAD67 neurotransmitter and Abeta. tha 35-42 synaptophysin Mus musculus 79-82 32473192-8 2020 Besides, the data represented that tacrine accelerated the expression of NR2B, SYP and GAD65 while it caused deceleration on the expression of GAD67 neurotransmitter and Abeta. tha 35-42 glutamic acid decarboxylase 2 Mus musculus 87-92 32473192-8 2020 Besides, the data represented that tacrine accelerated the expression of NR2B, SYP and GAD65 while it caused deceleration on the expression of GAD67 neurotransmitter and Abeta. tha 35-42 amyloid beta (A4) precursor protein Mus musculus 170-175 32360492-3 2020 In our synthetic work, we used "click-chemistry" to synthesize two Multi Target Directed Ligands (MTDLs) MB105 and MB118 carrying tacrine and quinuclidine scaffolds which are known for their anticholinesterase and alpha7 nicotinic acetylcholine receptor agonist activities, respectively. tha 130-137 cholinergic receptor nicotinic alpha 7 subunit Homo sapiens 214-253 33488178-2 2020 Food and Drug Administration (FDA) approved drugs donepezil, rivastigmine, tacrine and galantamine are AChE inhibitors and in the treatment of Alzheimer"s disease (AD) these drugs are currently prescribed. tha 75-82 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-107 32230733-4 2020 Comparing the protective efficacy of five such cholinesterase inhibitors (physostigmine, pyridostigmine, ranitidine, tacrine, or K-27), we observed best protection for the experimental oxime K-27. tha 117-124 butyrylcholinesterase Rattus norvegicus 47-61 32230733-4 2020 Comparing the protective efficacy of five such cholinesterase inhibitors (physostigmine, pyridostigmine, ranitidine, tacrine, or K-27), we observed best protection for the experimental oxime K-27. tha 117-124 keratin 27 Rattus norvegicus 191-195 31978679-3 2020 Compounds 4ah and 4bh proved to be more potent than the standard drug tacrine, rivastigmine and galantamine for AChE inhibition activity with IC50 value between 0.055 +- 0.143 microM and 0.017 +- 0.02 microM respectively. tha 70-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 112-116 32032848-0 2020 Tacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M1 muscarinic acetylcholine receptors. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-114 32032848-5 2020 The results were compared with those obtained on the known derivatives 6-C7 and 6-C10, two quite potent AChE inhibitors in which tacrine is linked to iperoxo, an exceptionally potent muscarinic orthosteric activator. tha 129-136 acetylcholinesterase (Cartwright blood group) Homo sapiens 104-108 32032848-0 2020 Tacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M1 muscarinic acetylcholine receptors. tha 23-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-114 32032848-2 2020 When tested in vitro in a colorimetric assay for their ability to inhibit AChE, the new compounds showed higher or similar potency compared to that of tacrine. tha 151-158 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 31996889-1 2020 A thermoresponsive NIPAAm-based polymer is combined with the selective acetylcholinesterase inhibitor tacrine in order to create a strict in sense on/off switch for enzymatic activity. tha 102-109 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-91 32679025-5 2020 Various cholinesterase inhibitors available in the market like Tacrine, Donepezil, Galantamine, Rivastigmine, etc are being used to manage the symptoms of Alzheimer"s disease. tha 63-70 butyrylcholinesterase Homo sapiens 8-22 31357051-0 2020 Colorimetric assay of acetylcholinesterase inhibitor tacrine based on MoO2 nanoparticles as peroxidase mimetics. tha 53-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-42 31357051-7 2020 In the presence of AChE inhibitor tacrine, the generation of TCh was inhibited and the absorbance was preserved. tha 34-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-23 31357051-8 2020 Based on these properties, a colorimetric assay method was developed for AChE inhibitor tacrine. tha 88-95 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 31666199-9 2020 Intact male GPR88 KO mice showed diminished tacrine-induced PD-like tremor and spontaneous hyperlocomotion. tha 44-51 G-protein coupled receptor 88 Mus musculus 12-17 31244052-2 2019 Tacrine, a potent acetylcholinesterase (AChE) inhibitor, was previously a prescribed clinical therapeutic agent for AD, but it was recently withdrawn because it caused widespread hepatotoxicity. tha 0-7 acetylcholinesterase Mus musculus 18-38 32986667-3 2020 OBJECTIVE: The aim of the current study was to evaluate the potential of two tacrine-donepezil hybrid molecules (TA8Amino and TAHB3), which are AChE inhibitors, to induce neurodifferentiation and neuritogenesis in SH-SY5Y cells. tha 77-84 acetylcholinesterase (Cartwright blood group) Homo sapiens 144-148 31556693-6 2019 These reactivators of acetylcholinesterase have balanced physicochemical properties, and should be able to cross the blood-brain barrier with a slightly lowered cytotoxicity profile compared to reference tacrine. tha 204-211 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-42 31009936-2 2019 Here, we present age-related alterations of acetylcholine levels after administration of the acetylcholinesterase inhibitor drug tacrine in normal mice. tha 129-136 acetylcholinesterase Mus musculus 93-113 31609608-1 2019 We have designed and synthesized a series of 14 hybrid molecules out of the cholinesterase (ChE) inhibitor tacrine and a benzimidazole-based human cannabinoid receptor subtype 2 (hCB2R) agonist and investigated them in vitro and in vivo. tha 107-114 butyrylcholinesterase Homo sapiens 92-95 30724803-3 2019 This study evaluated its effects on cocaine-reinforced and food-reinforced behaviors in rats, using the cholinesterase inhibitor tacrine as a comparator. tha 129-136 butyrylcholinesterase Rattus norvegicus 104-118 31228470-3 2019 Based on our derived 3D-QSAR model for the reversible AChE inhibitors, we designed and synthesized three novel compounds 8-10, joining the tacrine and aroylacrylic acid phenylamide moieties, with a longer methylene chain to target two distinct, toplogically separated anionic areas on the AChE. tha 139-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 54-58 31244052-2 2019 Tacrine, a potent acetylcholinesterase (AChE) inhibitor, was previously a prescribed clinical therapeutic agent for AD, but it was recently withdrawn because it caused widespread hepatotoxicity. tha 0-7 acetylcholinesterase Mus musculus 40-44 31281020-0 2019 Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer"s disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids. tha 130-137 butyrylcholinesterase Homo sapiens 16-30 31281020-0 2019 Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer"s disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids. tha 130-137 phosphodiesterase 4D Homo sapiens 35-40 31281020-1 2019 A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer"s disease (AD). tha 12-19 butyrylcholinesterase Homo sapiens 91-105 31281020-1 2019 A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer"s disease (AD). tha 12-19 butyrylcholinesterase Homo sapiens 107-110 31281020-1 2019 A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer"s disease (AD). tha 12-19 phosphodiesterase 4D Homo sapiens 116-136 31281020-1 2019 A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer"s disease (AD). tha 12-19 phosphodiesterase 4D Homo sapiens 138-143 31281020-2 2019 Compound 10j, which is tacrine linked with pyrazolo[3,4-b]pyridine moiety by a six-carbon spacer, was the most potent acetylcholinesterase (AChE) with IC50 value of 0.125 muM. tha 23-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 31281020-2 2019 Compound 10j, which is tacrine linked with pyrazolo[3,4-b]pyridine moiety by a six-carbon spacer, was the most potent acetylcholinesterase (AChE) with IC50 value of 0.125 muM. tha 23-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 140-144 30782574-0 2019 Chlorinated tacrine analogs: Design, synthesis and biological evaluation of their anti-cholinesterase activity as potential treatment for Alzheimer"s disease. tha 12-19 butyrylcholinesterase Homo sapiens 87-101 31158577-6 2019 Amongst them, 7k, 7m and 7p, all with a 6 carbon linker between tacrine and isatin Schiff base exhibited the strongest inhibitory activity against AChE with IC50 values of 0.42 nM, 0.62 nM and 0.95 nM, respectively. tha 64-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 31158577-7 2019 They were 92-, 62- and 41-fold more active than tacrine (IC50 = 38.72 nM) toward AChE. tha 48-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-85 31059278-0 2019 Potent Acetylcholinesterase Selective and Reversible Homodimeric Agent Based on Tacrine for Theranostics. tha 80-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 7-27 31170562-1 2019 A series of novel tacrine derivatives as multifunctional agents with potential inhibitory effects on both acetylcholinesterase(AChE) and butyrylcholinesterase (BuChE) enzymes for the treatment of Alzheimer"s disease(AD), were applied to alignment independent 3D-QSAR methods using Pentacle software. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 31170562-3 2019 Two H-bond acceptor groups as well as hydrophobic properties of tacrine rings for AChE and two H-bond acceptor on the carbonyl group of chromene and NH of amid group for BuChE, with positive effects on their inhibitory potency have been identified. tha 64-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 31125474-10 2019 Molecular docking was applied to postulate the selectivity toward AChE of 5a in comparison with donepezil and tacrine. tha 110-117 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 30782574-1 2019 In search of potent acetyl cholinesterase inhibitors with low hepatotoxicity for the treatment of Alzheimer"s disease, introduction of a chloro substitution to tacrine and some of its analogs has proven to be beneficial in maintaining or potentiating the cholinesterase inhibitory activity. tha 160-167 butyrylcholinesterase Homo sapiens 27-41 30782574-1 2019 In search of potent acetyl cholinesterase inhibitors with low hepatotoxicity for the treatment of Alzheimer"s disease, introduction of a chloro substitution to tacrine and some of its analogs has proven to be beneficial in maintaining or potentiating the cholinesterase inhibitory activity. tha 160-167 butyrylcholinesterase Homo sapiens 255-269 30851693-3 2019 For all the tacrine-tryptophan heterodimers, favorable inhibitory effect on hAChE as well as on hBChE was coined to the optimal spacer length ranging from five to eight carbon atoms between these two pharmacophores. tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-81 30849722-6 2019 Additionally, the IC50 of tacrine and ethopropazine for the inhibition of AChE and BChE were estimated to be 29.8 nM and 132.6 nM, respectively. tha 26-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-78 30849722-6 2019 Additionally, the IC50 of tacrine and ethopropazine for the inhibition of AChE and BChE were estimated to be 29.8 nM and 132.6 nM, respectively. tha 26-33 butyrylcholinesterase Homo sapiens 83-87 30798053-2 2019 Two scaffolds, targeting AChE (tacrine) and GSK-3alpha/beta (valmerin) simultaneously, were assembled, using copper(I)-catalysed azide alkyne cycloaddition (CuAAC), to generate a new series of multifunctional ligands. tha 31-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 25-29 30851693-3 2019 For all the tacrine-tryptophan heterodimers, favorable inhibitory effect on hAChE as well as on hBChE was coined to the optimal spacer length ranging from five to eight carbon atoms between these two pharmacophores. tha 12-19 butyrylcholinesterase Homo sapiens 96-101 30417195-8 2019 The inhibition test of tacrine on BChE with this assay substantiates its feasibility in screening potential inhibitors of BChE. tha 23-30 butyrylcholinesterase Homo sapiens 34-38 30391700-1 2019 A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer"s disease (AD) drug leads. tha 43-50 acetylcholinesterase Mus musculus 89-93 30391700-1 2019 A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer"s disease (AD) drug leads. tha 43-50 butyrylcholinesterase Mus musculus 94-116 30391700-1 2019 A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer"s disease (AD) drug leads. tha 43-50 butyrylcholinesterase Mus musculus 118-122 30391700-1 2019 A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer"s disease (AD) drug leads. tha 43-50 acetylcholinesterase Mus musculus 201-205 30391700-1 2019 A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the molecular docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer"s disease (AD) drug leads. tha 43-50 acetylcholinesterase Mus musculus 201-205 30468798-7 2019 In vivo experiments with acetylcholinesterase inhibitors donepezil and tacrine, as well as with the positive allosteric modulators of M4 receptor VU0152100 and VU0010010 show that this effect is sufficient to reverse the increased locomotor activity of DAT-knockout mice. tha 71-78 solute carrier family 6 (neurotransmitter transporter, dopamine), member 3 Mus musculus 253-256 30417195-8 2019 The inhibition test of tacrine on BChE with this assay substantiates its feasibility in screening potential inhibitors of BChE. tha 23-30 butyrylcholinesterase Homo sapiens 122-126 30319609-3 2018 Results: The results of this study showed that monocyte induced inflammation (raised tumor necrosis factor-alpha-TNF-alpha) induced by mCRP was significantly blocked in the presence of acetylcholine and nicotine, whilst tacrine and targeted antibodies (clones 8C10 and 3H12) had less of or no significant effects. tha 220-227 tumor necrosis factor Homo sapiens 85-112 31642410-2 2019 Oral treatment with tacrine hydrochloride; a reversible inhibitor of acetylcholinesterase, finds limited use in Alzheimer"s disease due to frequent dosing, hepatotoxicity and extensive pre-systemic metabolism. tha 20-41 acetylcholinesterase Rattus norvegicus 69-89 30343499-3 2018 Drugs, such as tacrine, rivastigmine, donepezil, and galantamine are known as acetylcholinesterase inhibitors. tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-98 30483056-0 2018 Tacrine(10)-Hupyridone Prevents Post-operative Cognitive Dysfunction via the Activation of BDNF Pathway and the Inhibition of AChE in Aged Mice. tha 0-7 brain derived neurotrophic factor Mus musculus 91-95 30483056-0 2018 Tacrine(10)-Hupyridone Prevents Post-operative Cognitive Dysfunction via the Activation of BDNF Pathway and the Inhibition of AChE in Aged Mice. tha 0-7 acetylcholinesterase Mus musculus 126-130 30483056-4 2018 In this study, we have discovered that tacrine(10)-hupyridone (A10E), a novel acetylcholinesterase (AChE) inhibitor derived from tacrine and huperzine A, could prevent surgery-induced short-term and long-term impairments of recognition and spatial cognition, as evidenced by the novel object recognition test and Morris water maze (MWM) tests, in aged mice. tha 39-46 acetylcholinesterase Mus musculus 78-98 30483056-4 2018 In this study, we have discovered that tacrine(10)-hupyridone (A10E), a novel acetylcholinesterase (AChE) inhibitor derived from tacrine and huperzine A, could prevent surgery-induced short-term and long-term impairments of recognition and spatial cognition, as evidenced by the novel object recognition test and Morris water maze (MWM) tests, in aged mice. tha 39-46 acetylcholinesterase Mus musculus 100-104 31679230-8 2019 Furthermore, IOP decreased the cytochrome c release and activation of caspase-3 induced by tacrine. tha 91-98 cytochrome c, somatic Homo sapiens 31-43 31679230-8 2019 Furthermore, IOP decreased the cytochrome c release and activation of caspase-3 induced by tacrine. tha 91-98 caspase 3 Homo sapiens 70-79 29278947-0 2018 Synthesis and bioevaluation of new tacrine-cinnamic acid hybrids as cholinesterase inhibitors against Alzheimer"s disease. tha 35-42 butyrylcholinesterase Homo sapiens 68-82 29624715-0 2018 Multifunctional properties of novel tacrine congeners: cholinesterase inhibition and cytotoxic activity. tha 36-43 butyrylcholinesterase Homo sapiens 55-69 30319609-3 2018 Results: The results of this study showed that monocyte induced inflammation (raised tumor necrosis factor-alpha-TNF-alpha) induced by mCRP was significantly blocked in the presence of acetylcholine and nicotine, whilst tacrine and targeted antibodies (clones 8C10 and 3H12) had less of or no significant effects. tha 220-227 C-reactive protein, pentraxin-related Mus musculus 135-139 30079554-3 2018 Monophenyl (16-18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37-57 nM and 84-93 nM, respectively, compared with their starting materials 15a-c and reference compounds (galanthamine and tacrine). tha 228-235 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 82-87 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 2B Homo sapiens 88-94 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 82-87 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 2C Homo sapiens 106-112 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 82-87 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 2D Homo sapiens 121-127 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 82-87 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 2A Homo sapiens 191-197 30099049-0 2018 7-Methoxyderivative of tacrine is a "foot-in-the-door" open-channel blocker of GluN1/GluN2 and GluN1/GluN3 NMDA receptors with neuroprotective activity in vivo. tha 23-30 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 79-84 30099049-0 2018 7-Methoxyderivative of tacrine is a "foot-in-the-door" open-channel blocker of GluN1/GluN2 and GluN1/GluN3 NMDA receptors with neuroprotective activity in vivo. tha 23-30 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 95-100 30099049-6 2018 We showed that both THA and 7-MEOTA are "foot-in-the-door" open-channel blockers of GluN1/GluN2 receptors and that 7-MEOTA is a more potent but slower blocker than THA. tha 20-23 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 84-89 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 1 Homo sapiens 64-69 30099049-7 2018 We found that the IC50 values for THA and 7-MEOTA exhibited the GluN1/GluN2A < GluN1/GluN2B < GluN1/GluN2C = GluN1/GluN2D relationship and that 7-MEOTA effectively inhibits human GluN1/GluN2A-M817V receptors that carry a pathogenic mutation. tha 34-37 glutamate ionotropic receptor NMDA type subunit 2A Homo sapiens 70-76 30079554-3 2018 Monophenyl (16-18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37-57 nM and 84-93 nM, respectively, compared with their starting materials 15a-c and reference compounds (galanthamine and tacrine). tha 228-235 butyrylcholinesterase Homo sapiens 73-77 29883670-7 2018 In concert with two prior studies, these results are suggestive of behavioral evidence for a biphasic effect of adenosine A2A receptor antagonists (caffeine and SCH 58261) that is modulated by tacrine, and a model of this effect is proposed. tha 193-200 adenosine A2a receptor Rattus norvegicus 112-134 29705288-4 2018 VEGF expression in the medial septal area was assessed by RT-PCR and immunostaining using mice treated with tacrine [9-amino-1,2,3,4-tetrahydro-acridine HCl (THA); 2.5 mg/kg, i.p.] tha 108-115 vascular endothelial growth factor A Mus musculus 0-4 30157868-8 2018 Tacrine lowered heart rate in male but not in female mice, induced higher plasma cTNI level and increased cardiac superoxide (DHE staining) generation in female than male mice, indicating stronger cardiac toxicity in female than male mice. tha 0-7 troponin I, cardiac 3 Mus musculus 81-85 29567174-5 2018 The model for AChE inhibition was further established and two traditional AChE inhibitors (donepezil and tacrine) were employed to verify the feasibility of the system. tha 105-112 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-18 29564727-1 2018 Tacrine(10)-hupyridone (A10E) was designed as a dual-binding acetylcholinesterase (AChE) inhibitor from the modification of tacrine and a fragment of huperzine A. tha 0-7 acetylcholinesterase Mus musculus 83-87 29564727-1 2018 Tacrine(10)-hupyridone (A10E) was designed as a dual-binding acetylcholinesterase (AChE) inhibitor from the modification of tacrine and a fragment of huperzine A. tha 124-131 acetylcholinesterase Mus musculus 83-87 29870588-6 2018 The most active compound 3d (IC50 = 7.6 pM for AChE and 1.7 pM for BuChE) appeared to be a much more active inhibitor than tacrine (IC50 = 89.9 nM for AChE and 14.9 nM for BuChE). tha 124-131 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 29870588-6 2018 The most active compound 3d (IC50 = 7.6 pM for AChE and 1.7 pM for BuChE) appeared to be a much more active inhibitor than tacrine (IC50 = 89.9 nM for AChE and 14.9 nM for BuChE). tha 124-131 acetylcholinesterase (Cartwright blood group) Homo sapiens 153-157 29635172-2 2018 In the present study, a surface plasmon resonance (SPR)-based assay was developed and employed to investigate interactions between human recombinant AChE (hAChE) and four known ligands: galantamine, tacrine, donepezil and edrophonium. tha 199-206 acetylcholinesterase (Cartwright blood group) Homo sapiens 149-153 29533874-1 2018 Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in vitro as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 221-226 29786716-2 2018 In the crystal structure of the BChE-tacrine complex, there is an unanticipated formyl-proline molecule resolved very close to tacrine, raising an essential question on how reliable it is to apply the binding pose in a crystal structure to analyze related experimental observations, in which no formyl-proline is actually involved. tha 37-44 butyrylcholinesterase Homo sapiens 32-36 29533874-1 2018 Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in vitro as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). tha 6-13 butyrylcholinesterase Homo sapiens 261-266 29533874-1 2018 Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in vitro as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). tha 48-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 221-226 29533874-1 2018 Novel tacrine-benzyl quinolone carboxylic acid (tacrine-BQCA) hybrids were designed based on multi-target directed ligands (MTLDs) paradigm, synthesized and evaluated in vitro as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). tha 48-55 butyrylcholinesterase Homo sapiens 261-266 29533874-4 2018 All the novel tacrine-BQCA hybrids were able to block the action of hAChE and hBChE in micromolar to nanomolar range. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-73 29533874-4 2018 All the novel tacrine-BQCA hybrids were able to block the action of hAChE and hBChE in micromolar to nanomolar range. tha 14-21 butyrylcholinesterase Homo sapiens 78-83 29298819-2 2018 The effects of systemic application of tacrine, an HNMT inhibitor, on the development of MS were observed. tha 39-46 histamine N-methyltransferase Rattus norvegicus 51-55 29390887-1 2018 Numerous studies show that tacrine derivatives exhibit increased inhibitory activity against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE). tha 27-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 149-153 29992880-0 2018 Tacrine-coumarin and Tacrine-7-chloroquinoline Hybrids with Thiourea Linkers: Cholinesterase Inhibition Properties, Kinetic Study, Molecular Docking and Permeability Assay for Blood-brain Barrier. tha 0-7 butyrylcholinesterase Homo sapiens 78-92 29281794-10 2018 Tacrine was identified as a potent NQO2 inhibitor and was applied to further confirm the catalytic activity of NQO2 in these assays. tha 0-7 N-ribosyldihydronicotinamide:quinone reductase 2 Homo sapiens 35-39 29281794-10 2018 Tacrine was identified as a potent NQO2 inhibitor and was applied to further confirm the catalytic activity of NQO2 in these assays. tha 0-7 N-ribosyldihydronicotinamide:quinone reductase 2 Homo sapiens 111-115 29268129-0 2018 Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. tha 15-22 butyrylcholinesterase Homo sapiens 58-72 28792233-8 2018 Also, tacrine inhibited AChE showed a Ki value of 446.56 +- 58.33 nM. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 24-28 28944565-1 2018 New synthesized series of 9-amino-1,2,3,4-tetrahydroacridine derivatives with iodobenzoic acid moiety were studied for their inhibitory activity toward cholinesterase and against beta-amyloid aggregation. tha 26-60 butyrylcholinesterase Homo sapiens 152-166 28646502-7 2018 In the validation study, coadministration with oral beta-glucuronidase derived from Escherichia coli and pretreatment with vancomycin and imipenem significantly modulated the susceptibility to tacrine-induced transaminitis in vivo. tha 193-200 glucuronidase, beta Rattus norvegicus 52-70 29149534-5 2018 Additionally, tacrine inhibited AChE and obtained a Ki value of 174.6 nM. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-36 29992880-8 2018 CONCLUSION: Tacrine-quinoline hybrids 7a exhibited the highest activity towards hBChE (IC50 = 0.97 micromol) and 7d towards hAChE (IC50 = 0.32 micromol). tha 12-19 butyrylcholinesterase Homo sapiens 80-85 29992880-8 2018 CONCLUSION: Tacrine-quinoline hybrids 7a exhibited the highest activity towards hBChE (IC50 = 0.97 micromol) and 7d towards hAChE (IC50 = 0.32 micromol). tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-129 28810188-0 2017 Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 28100082-7 2017 Additionally, tacrine showed Ki values of 25.75 +- 3.39 nM and 37.82 +- 2.08 against AChE and BChE, respectively. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 28100082-7 2017 Additionally, tacrine showed Ki values of 25.75 +- 3.39 nM and 37.82 +- 2.08 against AChE and BChE, respectively. tha 14-21 butyrylcholinesterase Homo sapiens 94-98 28133981-5 2017 Tacrine, which is the first acetylcholinesterase (AChE) inhibitor, has been selected as the ideal active fragment because of its simple structure, clear activity, and its superiority in the structural modification, thus it could be introduced into the overall molecular skeletons of the multi-target-directed anti-AD agents. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 28-48 28133981-5 2017 Tacrine, which is the first acetylcholinesterase (AChE) inhibitor, has been selected as the ideal active fragment because of its simple structure, clear activity, and its superiority in the structural modification, thus it could be introduced into the overall molecular skeletons of the multi-target-directed anti-AD agents. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 28803044-0 2017 New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer"s disease. tha 53-60 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 28803044-1 2017 A novel series of tacrine-like compounds 7a-u possessing a fused pyrazolo[1,2-b]phthalazine structure were designed and synthesized as potent and selective inhibitors of AChE. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 170-174 28544359-8 2017 Additionally, Tacrine inhibited AChE and BChE, showing Ki values of 397.03 +- 31.66 and 210.21 +- 15.98 nM, respectively. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-36 28544359-8 2017 Additionally, Tacrine inhibited AChE and BChE, showing Ki values of 397.03 +- 31.66 and 210.21 +- 15.98 nM, respectively. tha 14-21 butyrylcholinesterase Homo sapiens 41-45 28302511-0 2017 Design, synthesis and biological evaluation of multifunctional tacrine-curcumin hybrids as new cholinesterase inhibitors with metal ions-chelating and neuroprotective property. tha 63-70 butyrylcholinesterase Rattus norvegicus 95-109 28788095-1 2017 Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer"s disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 28788095-1 2017 Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer"s disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 28788095-1 2017 Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer"s disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. tha 9-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 28788095-4 2017 Another interesting class of AChE inhibitors represents Huprines, designed by merging two fragments of the known AChE inhibitors-THA and (-)-huperzine A. tha 129-132 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-33 28788095-4 2017 Another interesting class of AChE inhibitors represents Huprines, designed by merging two fragments of the known AChE inhibitors-THA and (-)-huperzine A. tha 129-132 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 28400237-3 2017 However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2. tha 9-16 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 174-180 28400237-6 2017 The hepatotoxic potential of tacrine derivatives was evaluated using recombinant cytochrome (CYP) P450 CYP1A2 and CYP3A4 enzymes. tha 29-36 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 103-109 28400237-6 2017 The hepatotoxic potential of tacrine derivatives was evaluated using recombinant cytochrome (CYP) P450 CYP1A2 and CYP3A4 enzymes. tha 29-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-120 28632402-6 2017 Biodistribution studies, in normal mice, showed that [18F]-IND1 was retained in the brain after 1 h. In vivo tacrine-blocking experiments indicated this uptake could be specifically due to AChE interaction. tha 109-116 NUBP iron-sulfur cluster assembly factor, mitochondrial Homo sapiens 59-63 28632402-6 2017 Biodistribution studies, in normal mice, showed that [18F]-IND1 was retained in the brain after 1 h. In vivo tacrine-blocking experiments indicated this uptake could be specifically due to AChE interaction. tha 109-116 acetylcholinesterase Mus musculus 189-193 28248535-1 2017 Bis(3)-tacrine is a dimeric AChE inhibitor derived from tacrine with a potential to treat Alzheimer"s disease. tha 7-14 acetylcholinesterase Rattus norvegicus 28-32 29349981-5 2017 Primary THA reasons:12 cases for DDH(9 cases for Crowe IV), 5 cases for femoral neck fracture, 2 cases for necrosis of femoral head, 2 cases for proximal femoral deformity caused by early infection. tha 8-11 aldo-keto reductase family 1 member C1 Homo sapiens 33-36 28125507-5 2017 Huprine X, a reversible AChE inhibitor, designed by molecular hybridization of tacrine and huperzine A, has been shown to affect the amyloidogenic process in vitro, and the AD-related neuropathology in vivo in mice models of the disease. tha 79-86 acetylcholinesterase Mus musculus 24-28 27876467-9 2017 This review describes differently synthesized tacrine-based scaffolds as cholinesterase inhibitors to manage Alzheimer"s disease (AD). tha 46-53 butyrylcholinesterase Homo sapiens 73-87 29332586-8 2017 We have demonstrated that this approach is possible, and that a number of readily available tacrine analogues show cholinesterase inhibition power, as well as other pharmacological properties, such as calcium channel blockade, antioxidant properties, neuroprotection, Abeta-amyloid inhibition aggregation capacity, etc., making them suitable multipotent molecules for further development for the potential treatment of AD. tha 92-99 butyrylcholinesterase Homo sapiens 115-129 28064079-3 2017 In a continuation of our efforts aimed at a new series of anti-AD MTDLs, we combined the structural features of the cholinesterase inhibitor drug tacrine with that of resveratrol, which is known for its purported antioxidant and anti-neuroinflammatory activities. tha 146-153 butyrylcholinesterase Homo sapiens 116-130 27998671-0 2017 Synthesis, physicochemical and biological studies of technetium-99m labeled tacrine derivative as a diagnostic tool for evaluation of cholinesterase level. tha 76-83 butyrylcholinesterase Homo sapiens 134-148 28040533-4 2017 Subsequent studies showed that tacrine was an acetylcholinesterase inhibitor. tha 31-38 acetylcholinesterase Canis lupus familiaris 46-66 28567126-6 2017 The hybrid compound containing the tryptoline moiety linked with a 7 carbon spacer to tacrine (14) displayed the best AChE and BuChE inhibitory activity (IC50 = 17.37 and 3.16 nM). tha 86-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-122 28294041-2 2017 In particular, tacrine, a well known Acetylcholinesterase inhibitor, is one of the most used starting point to develop multifunctional ligands and hundreds of papers report about these new agents. tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-57 27697055-9 2017 In particular, it focuses on THA hybrids capable of scavenging reactive oxygen species (ROS), and derivatives which reduce the formation of Abeta-plaques either directly by confronting the Abeta1-42 selfaggregation process or indirectly by inhibiting the BACE-1 enzyme or AChE-induced Abeta1-40 aggregation. tha 29-32 beta-secretase 1 Homo sapiens 255-261 27697055-9 2017 In particular, it focuses on THA hybrids capable of scavenging reactive oxygen species (ROS), and derivatives which reduce the formation of Abeta-plaques either directly by confronting the Abeta1-42 selfaggregation process or indirectly by inhibiting the BACE-1 enzyme or AChE-induced Abeta1-40 aggregation. tha 29-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 272-276 27988521-8 2017 Only tacrine was probably able to stereospecifically interact with the naturally occurring amyloid-beta isoform and to simultaneously stimulate CHT1. tha 5-12 solute carrier family 5 member 7 Rattus norvegicus 144-148 27055393-0 2016 Development of a biosensing system for tacrine based on nitrogen-doped graphene quantum dots and acetylcholinesterase. tha 39-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-117 27984137-11 2017 Also, AChE was inhibited by tacrine as an AChE inhibitor at the 71.18nM level. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 6-10 27984137-11 2017 Also, AChE was inhibited by tacrine as an AChE inhibitor at the 71.18nM level. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 27698319-1 2016 Crystallization of tacrine hydrochloride, an acetylcholinesterase inhibitor used during treatment of mild to moderate Alzheimer"s disease, from a water:ethanol solution has resulted in an orthorhombic pseudopolymorph. tha 19-40 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-65 27235273-0 2016 Tacrine-(hydroxybenzoyl-pyridone) hybrids as potential multifunctional anti-Alzheimer"s agents: AChE inhibition, antioxidant activity and metal chelating capacity. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-100 27235273-1 2016 Three novel potentially site-activated multitarget tacrine-(hydroxybenzoyl-pyridone) (TAC-HBP) hybrids were designed, synthesized and evaluated as acetylcholinesterase (AChE) inhibitors, antioxidants and biometal chelators. tha 51-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-167 27235273-1 2016 Three novel potentially site-activated multitarget tacrine-(hydroxybenzoyl-pyridone) (TAC-HBP) hybrids were designed, synthesized and evaluated as acetylcholinesterase (AChE) inhibitors, antioxidants and biometal chelators. tha 51-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 169-173 27230386-0 2016 Targeting copper(II)-induced oxidative stress and the acetylcholinesterase system in Alzheimer"s disease using multifunctional tacrine-coumarin hybrid molecules. tha 127-134 acetylcholinesterase (Cartwright blood group) Homo sapiens 54-74 27050248-6 2016 Also, Tacrine inhibited AChE and BChE showed Ki values of 396.03 and 209.21 nM, respectively. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 24-28 27050248-6 2016 Also, Tacrine inhibited AChE and BChE showed Ki values of 396.03 and 209.21 nM, respectively. tha 6-13 butyrylcholinesterase Homo sapiens 33-37 27484515-3 2016 In particular, compounds 29, 32 and 40 displayed inhibition at nano-molar level against AChE and BuChE (IC50s = 0.005-0.08 muM), being more potent than reference drug tacrine. tha 167-174 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-92 27392529-0 2016 Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach. tha 16-23 butyrylcholinesterase Homo sapiens 55-69 27392529-0 2016 Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach. tha 16-23 S100 calcium binding protein B Homo sapiens 91-96 27392529-3 2016 AChE molecular modeling studies of these hybrids indicated that tacrine moiety interacts in the bottom of the gorge with the catalytic active site (CAS) while tianeptine binds to peripheral anionic site (PAS). tha 64-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 27398906-6 2016 Perimidine molecule displayed promising inhibitory activity against acetylcholinesterase (AChE) as compared to the reference drug, tacrine. tha 131-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-88 27398906-6 2016 Perimidine molecule displayed promising inhibitory activity against acetylcholinesterase (AChE) as compared to the reference drug, tacrine. tha 131-138 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-94 27235273-2 2016 All of them are dual-binding site AChE inhibitors with activity in sub-micromolar range (IC50=0.57-0.78muM), which is comparable to the parent tacrine, and have good 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity (EC50=204-249muM) conferred by the hydroxybenzoyl-pyridone (HBP) moiety. tha 143-150 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-38 27618041-6 2016 Calibration of AChE inhibitors, tacrine and galantamine, was performed, with limit of detection equal to 1.1 nM and 1.28 microM, respectively. tha 32-39 acetylcholinesterase Mus musculus 15-19 27128182-6 2016 Thus, a new family of tacrine analogues, whose potent AChEI activity is linked to both their Abeta-aggregating and tau-phosphorylation inhibitory capacities, has been discovered for the potential treatment of AD. tha 22-29 microtubule associated protein tau Homo sapiens 115-118 27055393-1 2016 This work presents a novel fluorescent sensor for the determination of tacrine by combining the magnificent fluorescence properties of nitrogen-doped graphene quantum dots (N-GQDs) with the high potential of acetylcholinesterase (AChE) enzyme for screening its inhibitors. tha 71-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 208-228 27055393-1 2016 This work presents a novel fluorescent sensor for the determination of tacrine by combining the magnificent fluorescence properties of nitrogen-doped graphene quantum dots (N-GQDs) with the high potential of acetylcholinesterase (AChE) enzyme for screening its inhibitors. tha 71-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 230-234 27055393-2 2016 Tacrine was the first drug approved for Alzheimer"s disease and it is currently being used in several therapeutic treatments given its activity as a reversible inhibitor of AChE. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 173-177 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 143-164 albumin Homo sapiens 6-19 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 143-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 143-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 166-169 albumin Homo sapiens 6-19 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 166-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 26902639-1 2016 Human serum albumin (HSA) induced modulation of acetylcholinesterase (AChE) inhibition activity of four well-known cholinergic inhibitors like tacrine hydrochloride (TAC), donepezil hydrochloride monohydrate (DON), (-) Huperzine A (HuPA), eserine (ESE) was monitored quantitatively by Ellman"s method. tha 166-169 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 26861273-5 2016 In this work, we reported the synthesis and biological evaluation of a library of new tacrine-donepezil hybrids, as a potential dual binding site AChE inhibitor, containing a triazole-quinoline system. tha 86-93 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 26787846-4 2016 Using experimental mouse models of Parkinsonism, we report here that global p11 knockout (KO) mice develop fewer jaw tremors in response to tacrine. tha 140-147 S100 calcium binding protein A10 (calpactin) Mus musculus 76-79 26787846-7 2016 Selective deletion of p11 in cholinergic acetyltransferase (ChAT) neurons reduces tacrine-induced tremor. tha 82-89 S100 calcium binding protein A10 (calpactin) Mus musculus 22-25 26708634-0 2016 Effects of novel tacrine-related cholinesterase inhibitors in the reversal of 3-quinuclidinyl benzilate-induced cognitive deficit in rats--Is there a potential for Alzheimer"s disease treatment? tha 17-24 butyrylcholinesterase Rattus norvegicus 33-47 27075164-6 2016 Also, tacrine used as standard AChE inhibitor showed Ki value of 5.70 nM against AChE. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 31-35 27075164-6 2016 Also, tacrine used as standard AChE inhibitor showed Ki value of 5.70 nM against AChE. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-85 26558196-0 2015 The protective role of tacrine and donepezil in the retina of acetylcholinesterase knockout mice. tha 23-30 acetylcholinesterase Mus musculus 62-82 26503905-2 2015 Several of them showed improved inhibitory properties toward acetylcholinesterase (AChE) in relation to tacrine. tha 104-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-81 26503905-2 2015 Several of them showed improved inhibitory properties toward acetylcholinesterase (AChE) in relation to tacrine. tha 104-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 26650760-9 2015 Especially, we show that possible causes of Tacrine, donepezil, galantamine and huperzine A cannot improve the level of ACh which is against to their original design purpose but they still prevent AD to be worse as Abeta deposition appeared. tha 44-51 amyloid beta precursor protein Homo sapiens 215-220 25792506-0 2015 Tacrine-propargylamine derivatives with improved acetylcholinesterase inhibitory activity and lower hepatotoxicity as a potential lead compound for the treatment of Alzheimer"s disease. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 49-69 26558196-10 2015 CONCLUSION: In vivo, tacrine and donepezil can inhibit the expression of AChE; the decrease of AChE expression in the retina is beneficial for the development of the retina. tha 21-28 acetylcholinesterase Mus musculus 73-77 26558196-10 2015 CONCLUSION: In vivo, tacrine and donepezil can inhibit the expression of AChE; the decrease of AChE expression in the retina is beneficial for the development of the retina. tha 21-28 acetylcholinesterase Mus musculus 95-99 26438408-0 2015 Combined 3D-QSAR, molecular docking, and molecular dynamics study of tacrine derivatives as potential acetylcholinesterase (AChE) inhibitors of Alzheimer"s disease. tha 69-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-122 26438408-0 2015 Combined 3D-QSAR, molecular docking, and molecular dynamics study of tacrine derivatives as potential acetylcholinesterase (AChE) inhibitors of Alzheimer"s disease. tha 69-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-128 26438408-2 2015 Tacrine is an approved drug with AChE-inhibitory activity. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 33-37 26438408-3 2015 In this paper, 3D-QSAR, molecular docking, and molecular dynamics were carried out in order to study 60 tacrine derivatives and their AChE-inhibitory activities. tha 104-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 26194093-2 2015 We found, for the first time, that bis(heptyl)-cognitin, a novel dimeric acetylcholinesterase (AChE) inhibitor derived from tacrine, prevented Abeta oligomers-induced inhibition of long-term potentiation (LTP) at concentrations that did not interfere with normal LTP. tha 124-131 acetylcholinesterase Mus musculus 95-99 25773602-6 2015 Moreover, elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in tacrine-treated mice were significantly reduced after oral administration of fucosterol. tha 97-104 glutamic pyruvic transaminase, soluble Mus musculus 19-43 25773602-6 2015 Moreover, elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in tacrine-treated mice were significantly reduced after oral administration of fucosterol. tha 97-104 glutamic pyruvic transaminase, soluble Mus musculus 45-48 25773602-6 2015 Moreover, elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in tacrine-treated mice were significantly reduced after oral administration of fucosterol. tha 97-104 solute carrier family 17 (anion/sugar transporter), member 5 Mus musculus 54-80 25773602-6 2015 Moreover, elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in tacrine-treated mice were significantly reduced after oral administration of fucosterol. tha 97-104 solute carrier family 17 (anion/sugar transporter), member 5 Mus musculus 82-85 25969170-2 2015 The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE and BuChE, revealed that compounds bearing piperidinylethoxy residue showed potent activity against AChE at sub-micromolar level (IC50 values = 0.122-0.207 muM), more potent than reference drug tacrine. tha 276-283 acetylcholinesterase (Cartwright blood group) Homo sapiens 182-186 25269683-2 2015 Using the 3M APR-DRG severity of illness index as a measure of patient"s health status, we found a significant increase in cost for both TKA and THA for patients with higher severity of illness index. tha 145-148 phorbol-12-myristate-13-acetate-induced protein 1 Homo sapiens 13-16 25858345-3 2015 Tacrine, the first of the cholinesterase inhibitors to undergo extensive trials for this purpose, was associated with significant adverse effects including hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 26-40 25462245-1 2015 A new series of tacrine-based acetylcholinesterase (AChE) inhibitors 7a-l were designed by replacing the benzene ring of tacrine with aryl-dihydropyrano[2,3-c]pyrazole. tha 16-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-56 25747977-0 2015 Tacrine, an oral acetylcholinesterase inhibitor, induced hepatic oxidative damage, which was blocked by liquiritigenin through GSK3-beta inhibition. tha 0-7 acetylcholinesterase Rattus norvegicus 17-37 25747977-0 2015 Tacrine, an oral acetylcholinesterase inhibitor, induced hepatic oxidative damage, which was blocked by liquiritigenin through GSK3-beta inhibition. tha 0-7 glycogen synthase kinase 3 beta Rattus norvegicus 127-136 25747977-1 2015 Although the cholinesterase inhibitor tacrine has been successfully used for the treatment of Alzheimer"s disease, it is known to have hepatotoxic effects. tha 38-45 butyrylcholinesterase Rattus norvegicus 13-27 25747977-6 2015 Furthermore, LQ promoted inhibitory phosphorylation of glycogen synthase kinase-3beta (GSK3beta) and prevented decreases in GSK3beta phosphorylation induced by tacrine. tha 160-167 glycogen synthase kinase 3 beta Rattus norvegicus 124-132 24764253-4 2015 For comparison, the reference AChE inhibitors, tacrine and ranitidine, exhibit IC(50) values of 0.144 microM and 3.37 microM, respectively. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 26061104-5 2015 CONCLUSION: A new family of nonhepatotoxic showing selective acetylcholinesterase inhibition, permeable tacrine analogs have been discovered for the potential treatment of Alzheimer"s disease. tha 104-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-81 25682206-0 2015 THA Retrievals: The Need to Mark the Anatomic Orientation of the Femoral Head. tha 0-3 microtubule affinity regulating kinase 1 Homo sapiens 28-32 25812965-0 2015 Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer"s disease. tha 13-20 butyrylcholinesterase Homo sapiens 39-53 25812965-0 2015 Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer"s disease. tha 13-20 monoamine oxidase B Homo sapiens 58-77 25563372-8 2015 Kinetic studies showed that GNDAs were able to inhibit AChE by the same mode as tacrine (9-amino-1,2,3,4-tetrahydroacridine), a known inhibitor of AChE. tha 80-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 25563372-8 2015 Kinetic studies showed that GNDAs were able to inhibit AChE by the same mode as tacrine (9-amino-1,2,3,4-tetrahydroacridine), a known inhibitor of AChE. tha 89-123 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151 24706520-2 2014 However, tacrine-6-ferulic acid (T6FA), the dimer which added ferulic acid to tacrine, has been found to be a promising multifunctional drug candidate for AD and much more potent and selective on acetylcholinesterase (AChE) than tacrine. tha 9-16 acetylcholinesterase Rattus norvegicus 218-222 26228694-4 2015 RESULTS: We report that donepezil, memantine, dimebon, Pre-084 and 4-IBP are neuritogenic while tacrine, rosemarinic acid, memoquin and a BACE1 inhibitor suppress neurite outgrowth of neurons. tha 96-103 trafficking protein particle complex subunit 9 Homo sapiens 69-72 25265240-6 2014 The number of c-Fos-positive cells was significantly enhanced in the medial striatum, nucleus accumbens core, and nucleus accumbens shell after tacrine administration, and the enhanced expression of c-Fos in these three regions was significantly attenuated by cabergoline, while rotigotine suppressed c-Fos expression in two regions except the nucleus accumbens core. tha 144-151 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 14-19 25445524-1 2014 Tacrine (THA), as the first approved acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer"s disease (AD), has been extensively investigated in last seven decades. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-57 25445524-1 2014 Tacrine (THA), as the first approved acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer"s disease (AD), has been extensively investigated in last seven decades. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 25445524-1 2014 Tacrine (THA), as the first approved acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer"s disease (AD), has been extensively investigated in last seven decades. tha 9-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 37-57 25445524-1 2014 Tacrine (THA), as the first approved acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer"s disease (AD), has been extensively investigated in last seven decades. tha 9-12 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-63 25445524-4 2014 According to IC50 values, the in vitro anti-AChE activities of THA dimers were up to 300-fold more potent and 200-fold more selective than that of THA. tha 63-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-48 25445524-5 2014 In addition, the anti-AChE activities of THA dimers were found to be associated with the type and length of the linkage. tha 41-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 24890882-4 2014 As cholinergic approach has widely been practiced for the restoration of memory in various neurodegenerative disorders, this study was envisaged to evaluate add on effect of acetylcholinesterase inhibitor (tacrine) with phenytoin in pentylenetetrazole-kindling-induced learning and memory deficit in mice. tha 206-213 acetylcholinesterase Mus musculus 174-194 24136594-7 2014 Best in vivo protection from terbufos sulfone-induced mortality was achieved, when K-27 was given before terbufos sulfone exposure (RR = 0.06), which was significantly (P <= 0.05) superior to the pre-treatment with all other tested compounds, for example tacrine (RR = 0.21), pyridostigmine (RR = 0.28), physostigmine (RR = 0.29) and ranitidine (RR = 0.33). tha 258-265 keratin 27 Rattus norvegicus 83-87 25239202-0 2014 QSAR analysis on tacrine-related acetylcholinesterase inhibitors. tha 17-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 33-53 25239202-2 2014 The study of tacrine analogs presents a continuous interest, and for this reason we establish Quantitative Structure-Activity Relationships on their Acetylcholinesterase inhibitory activity. tha 13-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 149-169 25239202-3 2014 RESULTS: Ten groups of new developed Tacrine-related inhibitors are explored, which have been experimentally measured in different biochemical conditions and AChE sources. tha 37-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 158-162 25088549-2 2014 As the first acetylcholinesterase inhibitor approved for the clinical treatment of AD, tacrine has been widely used as a pharmacophore to design hybrid compounds in order to combine its potent AChE inhibition with other multi-target profiles. tha 87-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 13-33 25088549-2 2014 As the first acetylcholinesterase inhibitor approved for the clinical treatment of AD, tacrine has been widely used as a pharmacophore to design hybrid compounds in order to combine its potent AChE inhibition with other multi-target profiles. tha 87-94 acetylcholinesterase (Cartwright blood group) Homo sapiens 193-197 25088549-3 2014 In present study, a series of novel tacrine-coumarin hybrids were designed, synthesized and evaluated as potent dual-site AChE inhibitors. tha 36-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 122-126 25036600-2 2014 The most potent AChE inhibitor was found to be homodimeric tacrine derivative 14a, which demonstrated an IC50 value of 2 nM; this value indicates an activity rate which is 250-times higher than that of tacrine 1 and 7500-times higher than 7-MEOTA 15, the compounds which were used as standards in the study. tha 59-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-20 25036600-2 2014 The most potent AChE inhibitor was found to be homodimeric tacrine derivative 14a, which demonstrated an IC50 value of 2 nM; this value indicates an activity rate which is 250-times higher than that of tacrine 1 and 7500-times higher than 7-MEOTA 15, the compounds which were used as standards in the study. tha 202-209 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-20 24911952-6 2014 The rescuing effect of THA was also partially but significantly blocked by Ki8751, a selective inhibitor of type 2 vascular endothelial growth factor (VEGF) receptor (VEGFR-2) tyrosine kinase. tha 23-26 vascular endothelial growth factor A Homo sapiens 151-155 24911952-6 2014 The rescuing effect of THA was also partially but significantly blocked by Ki8751, a selective inhibitor of type 2 vascular endothelial growth factor (VEGF) receptor (VEGFR-2) tyrosine kinase. tha 23-26 kinase insert domain receptor Homo sapiens 167-174 24911952-11 2014 In OHSCs pretreated with NMDA, THA treatment induced a morphological and activation-related change in astrocytes expressing VEGF-A. tha 31-34 vascular endothelial growth factor A Homo sapiens 124-130 24895330-5 2014 Using structure-based design, we synthesized several azobenzene analogues of the well-known AChE inhibitor tacrine (THA) and determined their effects on enzymatic activity. tha 107-114 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 24560791-9 2014 Pretreatment with CA-074Me, a specific cathepsin B inhibitor resulted in a significant but not complete decrease in tacrine-induced apoptosis. tha 116-123 cathepsin B Homo sapiens 39-50 24560791-6 2014 Our results demonstrated that THA induced dose-dependent apoptosis with cytochrome c release and activation of caspase-3. tha 30-33 cytochrome c, somatic Homo sapiens 72-84 24560791-6 2014 Our results demonstrated that THA induced dose-dependent apoptosis with cytochrome c release and activation of caspase-3. tha 30-33 caspase 3 Homo sapiens 111-120 24560791-8 2014 In addition, we observed that THA led to an early lysosomal membrane permeabilization and release of cathepsin B. tha 30-33 cathepsin B Homo sapiens 101-112 24508831-3 2014 Molecular modeling studies revealed that these tacrine-carbazole hybrids interacted simultaneously with the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. tha 47-54 acetylcholinesterase Mus musculus 177-181 24095756-1 2013 A new series of tacrine-flavonoid hybrids (13a-u) had been designed, synthesized, and evaluated as multifunctional cholinesterase (ChE) inhibitors against Alzheimer"s disease (AD). tha 16-23 butyrylcholinesterase Homo sapiens 115-129 24310227-3 2014 Compound 10b was one of the most potent inhibitors and was 5-fold more active than tacrine toward AChE, and it also showed a moderate BuChE inhibition with an IC50 value of 200 nM. tha 83-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-102 24343873-0 2014 Novel tacrine analogs as potential cholinesterase inhibitors in Alzheimer"s disease. tha 6-13 butyrylcholinesterase Homo sapiens 35-49 24343873-4 2014 In this paper, we synthesized new tacrine analogs to act on catalytic and peripheral sites of AChE. tha 34-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 24910237-3 2014 The metabolic pathways examined were the CYP1A2-catalyzed tacrine 1-hydroxylation, CYP2B6-catalyzed bupropion hydroxylation, CYP2C8-catalyzed amodiaquine N-deethylation, CYP2C9- catalyzed diclofenac 4"-hydroxylation, CYP2D6-catalyzed dextromethorphan O-demethylation, and CYP3A4-catalyzed midazolam 1"-hydroxylation. tha 58-65 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 41-47 25117054-3 2014 Of these nine compounds, 4 and 7 showed hepatoprotective effects towards tacrine-induced cytotoxicity in Hep 3B cells with EC50 values of 42.7 +- 1.5 and 132.6 +- 2.8 muM, respectively. tha 73-80 latexin Homo sapiens 167-170 24186541-1 2013 This study presents the synthesis of 15 new tacrine dimers as well as the Ki and IC50 results, studies of the kinetic mechanism, and molecular docking analysis of the dimers in relation to the cholinesterases hAChE, hBChE, EeAChE and eqBChE. tha 44-51 butyrylcholinesterase Homo sapiens 216-221 24333766-8 2014 It can be inferred from data, that compound (6) showed potent AChE inhibition having IC50=0.27muM, almost in vicinity to reference drug Tacrine (IC50=0.19muM). tha 136-143 acetylcholinesterase Bos taurus 62-66 24128814-0 2013 Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. tha 65-72 butyrylcholinesterase Homo sapiens 14-28 24128814-0 2013 Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. tha 65-72 monoamine oxidase B Homo sapiens 33-52 24095756-1 2013 A new series of tacrine-flavonoid hybrids (13a-u) had been designed, synthesized, and evaluated as multifunctional cholinesterase (ChE) inhibitors against Alzheimer"s disease (AD). tha 16-23 butyrylcholinesterase Homo sapiens 131-134 23679855-0 2013 Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer"s drugs targeting acetyl- and butyryl-cholinesterase. tha 74-81 butyrylcholinesterase Homo sapiens 28-42 24096962-2 2013 The activity of HSD11B1 is measured in the urine based on the (tetrahydrocortisol+5alpha-tetrahydrocortisol)/tetrahydrocortisone ((THF+5alpha-THF)/THE) ratio in humans and the (tetrahydrocorticosterone+5alpha-tetrahydrocorticosterone)/tetrahydrodehydrocorticosterone ((THB+5alpha-THB)/THA) ratio in mice. tha 285-288 hydroxysteroid 11-beta dehydrogenase 1 Homo sapiens 16-23 23679855-2 2013 Such MTDLs are usually on the basis of cholinesterase inhibitors (e.g. tacrine or huprine) coupled with another active molecule aimed at a different target. tha 71-78 butyrylcholinesterase Homo sapiens 39-53 23679855-3 2013 To aid in the design of these MTDLs, we report the crystal structures of hAChE (human acetylcholinesterase) in complex with FAS-2 (fasciculin 2) and a hydroxylated derivative of huprine (huprine W), and of hBChE (human butyrylcholinesterase) in complex with tacrine. tha 258-265 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-78 23679855-4 2013 Huprine W in hAChE and tacrine in hBChE reside in strikingly similar positions highlighting the conservation of key interactions, namely, pi-pi/cation-pi interactions with Trp86 (Trp82), and hydrogen bonding with the main chain carbonyl of the catalytic histidine residue. tha 23-30 butyrylcholinesterase Homo sapiens 34-39 23768661-2 2013 In search for multifunctional anti-AD drug candidates, taking into account that the acetylcholinesterase (AChE) and beta-amyloid (Abeta) aggregation are particularly important targets for inhibition, the tacrine and benzothiazole (BTA) moieties were conjugated with suitable linkers in a novel series of hybrids. tha 204-211 amyloid beta precursor protein Homo sapiens 130-135 23768661-4 2013 All the tacrine-BTA hybrids displayed high in vitro activities, namely with IC50 values in the low micromolar to sub-micromolar concentration range towards the inhibition of AChE, and high percentages of inhibition of the self-induced Abeta aggregation. tha 8-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 174-178 23535563-2 2013 One strategy currently being explored for the development of new therapeutics for AD involves linking tacrine, a known acetylcholinesterase (AChE) inhibitor, to another drug to create bifunctional hybrids. tha 102-109 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-139 23740645-3 2013 The change in potency with tether length was high in DmAChE and low in BgAChE, associated with 90-fold and 5.2-fold maximal potency gain, respectively, compared to the tacrine monomer. tha 168-175 Acetylcholine esterase Drosophila melanogaster 53-59 23535563-2 2013 One strategy currently being explored for the development of new therapeutics for AD involves linking tacrine, a known acetylcholinesterase (AChE) inhibitor, to another drug to create bifunctional hybrids. tha 102-109 acetylcholinesterase (Cartwright blood group) Homo sapiens 141-145 23435942-6 2013 This review discusses the different classes of cholinesterase inhibitors including tacrine, donepezil, rivastigmine, galantamine, xanthostigmine, para-aminobenzoic acid, coumarin, flavonoid, and pyrrolo-isoxazole analogues developed for the treatment of AD. tha 83-90 butyrylcholinesterase Homo sapiens 47-61 23676090-6 2013 These findings identified beta-naphthotacrine10 as a potent and selective hAChE inhibitor in a nanomolar range, with toxicity lower than that of tacrine both in human hepatocytes and rat cortical neurons, with a potent neuroprotective activity and, consequently, an attractive multipotent active molecule of potential application in AD treatment. tha 38-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 74-79 23685572-0 2013 Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer"s disease. tha 42-49 butyrylcholinesterase Homo sapiens 86-100 23685572-1 2013 A series of tacrine-coumarin hybrids (8a-t) were designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against Alzheimer"s disease (AD). tha 12-19 butyrylcholinesterase Homo sapiens 104-118 23685572-1 2013 A series of tacrine-coumarin hybrids (8a-t) were designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against Alzheimer"s disease (AD). tha 12-19 butyrylcholinesterase Homo sapiens 120-123 24325732-3 2013 These heterodimers exhibit selectivity toward BuChE, being from 4- to 256-fold more active toward BuChE than AChE, but still acting as better AChE inhibitors than tacrine 4. tha 163-170 butyrylcholinesterase Homo sapiens 46-51 23618192-4 2013 Tacrine, a BChE inhibitor, was used as a positive reference compound, and its detection limit in the biochemical detection system was 1 nmol. tha 0-7 butyrylcholinesterase Homo sapiens 11-15 23618192-5 2013 The BChE activity of 1g of P. nelumbinis sample was equal to that of 127.88 mumol tacrine. tha 82-89 butyrylcholinesterase Homo sapiens 4-8 23639542-0 2013 NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. tha 12-19 butyrylcholinesterase Homo sapiens 45-66 23639542-2 2013 It was found that all the new target compounds showed selective butyrylcholinesterase (BuChE) inhibitory activity in vitro comparable or higher than tacrine and the tacrine-flurbiprofen hybrid compounds 1a-c, and released moderate amount of NO in vitro. tha 149-156 butyrylcholinesterase Homo sapiens 87-92 23639542-2 2013 It was found that all the new target compounds showed selective butyrylcholinesterase (BuChE) inhibitory activity in vitro comparable or higher than tacrine and the tacrine-flurbiprofen hybrid compounds 1a-c, and released moderate amount of NO in vitro. tha 165-172 butyrylcholinesterase Homo sapiens 64-85 23639542-2 2013 It was found that all the new target compounds showed selective butyrylcholinesterase (BuChE) inhibitory activity in vitro comparable or higher than tacrine and the tacrine-flurbiprofen hybrid compounds 1a-c, and released moderate amount of NO in vitro. tha 165-172 butyrylcholinesterase Homo sapiens 87-92 23494216-0 2013 Purification of acetylcholinesterase by 9-amino-1,2,3,4-tetrahydroacridine from human erythrocytes. tha 40-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-36 23494216-2 2013 Tacrine (9-amino-1,2,3,4-tetrahydroacridine) is a well-known drug for the treatment of Alzheimer"s disease, which inhibits cholinesterase. tha 0-7 butyrylcholinesterase Homo sapiens 123-137 23494216-2 2013 Tacrine (9-amino-1,2,3,4-tetrahydroacridine) is a well-known drug for the treatment of Alzheimer"s disease, which inhibits cholinesterase. tha 9-43 butyrylcholinesterase Homo sapiens 123-137 23454517-0 2013 A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer"s disease. tha 18-25 butyrylcholinesterase Homo sapiens 50-64 23422935-0 2013 Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors. tha 13-20 butyrylcholinesterase Homo sapiens 114-135 23454517-1 2013 A novel series of tacrine-selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). tha 18-25 butyrylcholinesterase Homo sapiens 108-122 23422935-1 2013 A novel series of tacrine-lophine hybrids was synthesized and tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 in the nanomolar concentration scale. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 98-118 23422935-1 2013 A novel series of tacrine-lophine hybrids was synthesized and tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 in the nanomolar concentration scale. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 120-124 23454517-1 2013 A novel series of tacrine-selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 124-128 23422935-1 2013 A novel series of tacrine-lophine hybrids was synthesized and tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 in the nanomolar concentration scale. tha 18-25 butyrylcholinesterase Homo sapiens 130-151 23422935-1 2013 A novel series of tacrine-lophine hybrids was synthesized and tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 in the nanomolar concentration scale. tha 18-25 butyrylcholinesterase Homo sapiens 153-158 23454517-1 2013 A novel series of tacrine-selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). tha 18-25 monoamine oxidase A Homo sapiens 159-166 23330848-4 2013 The assay method was validated using the reference AChE inhibitors tacrine and galanthamine. tha 67-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-55 23459299-0 2013 New tacrine analogs as acetylcholinesterase inhibitors - theoretical study with chemometric analysis. tha 4-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-43 22391555-7 2013 The use of AChE-ICER in the ligands recognition assay was validated by evaluation of four known reversible inhibitors (galanthamine, tacrine, propidium, and rivastigmine), and the same order of inhibitory potencies described in the literature was found. tha 133-140 acetylcholinesterase (Cartwright blood group) Homo sapiens 11-15 22391555-7 2013 The use of AChE-ICER in the ligands recognition assay was validated by evaluation of four known reversible inhibitors (galanthamine, tacrine, propidium, and rivastigmine), and the same order of inhibitory potencies described in the literature was found. tha 133-140 cAMP responsive element modulator Homo sapiens 16-20 23220711-8 2013 The effect of tacrine was induced in a manner dependent on the incubation period after NMDA treatment and was confirmed by Nissl staining and immunostaining with NeuN, a marker of mature neurons. tha 14-21 RNA binding protein, fox-1 homolog (C. elegans) 3 Mus musculus 162-166 23073222-5 2012 The models revealed the importance of protonated pyridine nitrogen of tacrine moiety for anti AChE activity, and recognized HBA and HBD interactions as highly important for the potency. tha 70-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 22818849-1 2012 New tacrine derivatives 5a-d, 6a-d with piperazino-ethyl spacer linked with corresponding secondary amines and tacrine homodimer 8 were synthesized and tested as cholinesterase inhibitors on human acetylcholinesterase (hAChE) and human plasmatic butyrylcholinesterase (hBChE). tha 4-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 219-224 22818849-1 2012 New tacrine derivatives 5a-d, 6a-d with piperazino-ethyl spacer linked with corresponding secondary amines and tacrine homodimer 8 were synthesized and tested as cholinesterase inhibitors on human acetylcholinesterase (hAChE) and human plasmatic butyrylcholinesterase (hBChE). tha 4-11 butyrylcholinesterase Homo sapiens 269-274 22818849-2 2012 In most cases the majority of synthesized derivatives exhibit a high AChE and BChE inhibitory activity with IC(50) values in the low-nanomolar range, being clearly more potent than the reference standard tacrine (9-amino-1,2,3,4-tetrahydroacridine, 1) and 7-MEOTA (7-methoxy-9-amino-1,2,3,4-tetrahydroacridine). tha 204-211 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-73 22818849-2 2012 In most cases the majority of synthesized derivatives exhibit a high AChE and BChE inhibitory activity with IC(50) values in the low-nanomolar range, being clearly more potent than the reference standard tacrine (9-amino-1,2,3,4-tetrahydroacridine, 1) and 7-MEOTA (7-methoxy-9-amino-1,2,3,4-tetrahydroacridine). tha 204-211 butyrylcholinesterase Homo sapiens 78-82 23931443-1 2013 Tacrine (1) was the first acetylcholinesterase inhibitor (AChEI) introduced in therapy for the treatment of Alzheimer"s disease (AD), but similarly to the most recent approved AChEIs and memantine, an N-methyl-D-aspartate receptor (NMDAR) antagonist, it does not represent an effective drug in halting the progression of AD. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-46 22944335-0 2012 O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-beta aggregation. tha 35-42 butyrylcholinesterase Homo sapiens 121-135 22944335-0 2012 O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-beta aggregation. tha 35-42 amyloid beta precursor protein Homo sapiens 149-161 22944335-3 2012 All of the hybrids are potential biometal chelators, and in addition, most of them were better antioxidants and inhibitors of cholinesterases and amyloid-beta (Abeta) aggregation than the lead compound tacrine. tha 202-209 amyloid beta precursor protein Homo sapiens 146-158 23256654-5 2012 Tacrine (9-amino-1,2,3,4-tetrahydroacridine) was the first cholinesterase inhibitor approved for symptomatic AD treatment. tha 0-7 butyrylcholinesterase Homo sapiens 59-73 23256654-5 2012 Tacrine (9-amino-1,2,3,4-tetrahydroacridine) was the first cholinesterase inhibitor approved for symptomatic AD treatment. tha 9-43 butyrylcholinesterase Homo sapiens 59-73 22613808-5 2012 The cytotoxicity of tacrine to HepG2 cells was associated with upregulations of Fas and JNK phosphorylation resulted in the caspase activations and apoptosis. tha 20-27 mitogen-activated protein kinase 8 Homo sapiens 88-91 22613808-7 2012 In addition, treatment of phlorofucofuroeckol A regulated the release of cytochrome c from mitochondria to cytosol in a dose-dependent manner in tacrine-treated HepG2 cells. tha 145-152 cytochrome c, somatic Homo sapiens 73-85 22613808-8 2012 Furthermore, pretreatment of an inhibitor of JNK, SP600125, downregulated Fas and cleaved caspase-3 without change of ROS productions in tacrine-treated HepG2 cells. tha 137-144 mitogen-activated protein kinase 8 Homo sapiens 45-48 22613808-9 2012 In conclusion, our study demonstrated that phlorofucofuroeckol A regulates Fas-mediated apoptosis via inhibition of ROS productions and inhibition of JNK phosphorylation in tacrine-treated HepG2 cells. tha 173-180 mitogen-activated protein kinase 8 Homo sapiens 150-153 23227542-4 2012 The results showed that icariin could potently inhibit the activity of AChE, the IC50 value was determined to be 3.50 x 10(-8) mol x L(-1), and the determined IC50 value to tacrine was 0.75 x 10(-8) mol x L(-1). tha 173-180 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-75 22359054-6 2012 The uptake of [(3)H]ALCAR by TR-BBB cells was inhibited by AChE inhibitors such as donepezil, tacrine, galantamine and rivastigmine, which IC(50) values are 45.3, 74.0, 459 and 800 muM, respectively. tha 94-101 acetylcholinesterase Rattus norvegicus 59-63 21621296-3 2012 Treatment of SH-SY5Y cells with the AChE-inhibitor tacrine decreased PS1 levels, in parallel with increase in the secretion of amyloid precursor protein APPalpha, whereas the cholinergic agonist carbachol had no effect on PS1. tha 51-58 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 22587607-5 2012 Both eckol and 2-phloroeckol inhibited the expression of Fas-mediated cell-death proteins, including tBid, caspase-3, and poly(ADP-ribose) polymerase, and suppressed the release of cytochrome c from mitochondria to cytosol in a dose-dependent manner in tacrine-treated HepG2 cells. tha 253-260 cytochrome c, somatic Homo sapiens 181-193 22739210-6 2012 The apparent total body activities of 11beta-HSD1 and 11beta-HSD2 were estimated using the urinary and plasma ratios of (THB+5alpha-THB)/THA and B/A. tha 137-140 hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 5 Rattus norvegicus 38-65 22624880-8 2012 The tacrine-silibinin codrug shows high AChE and BChE inhibition, neuroprotective effects, lacks tacrine"s hepatotoxicity in vitro and in vivo, and shows the same pro-cognitive effects in vivo as tacrine, being superior to the physical mixture of tacrine and silibinin in all these regards. tha 4-11 acetylcholinesterase Rattus norvegicus 40-44 22624880-8 2012 The tacrine-silibinin codrug shows high AChE and BChE inhibition, neuroprotective effects, lacks tacrine"s hepatotoxicity in vitro and in vivo, and shows the same pro-cognitive effects in vivo as tacrine, being superior to the physical mixture of tacrine and silibinin in all these regards. tha 4-11 butyrylcholinesterase Rattus norvegicus 49-53 22512543-1 2012 In search of multifunctional cholinesterase inhibitors as potential anti-Alzheimer drug candidates, tacrine-ferulic acid-NO donor trihybrids were synthesized and tested for their cholinesterase inhibitory activities, release of nitric oxide, vasodilator properties, cognition improving potency, and hepatotoxicity. tha 100-107 butyrylcholinesterase Mus musculus 29-43 22472046-0 2012 Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids. tha 104-111 butyrylcholinesterase Homo sapiens 14-28 22472046-2 2012 Compound 44b, tacrine linked with phenyl-benzothiazole by 3-carbon spacers, was the most potent AChE inhibitor with an IC(50) value of 0.017 muM. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 96-100 22472693-2 2012 Previously our group has reported a series of tacrine-based hybrids as potent AChE inhibitors (AChEI). tha 46-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 22192081-1 2012 Tacrine is an acetylcholinesterase (AChE) inhibitor used as a cognitive enhancer in the treatment of Alzheimer"s disease (AD). tha 0-7 acetylcholinesterase Rattus norvegicus 14-34 22192081-1 2012 Tacrine is an acetylcholinesterase (AChE) inhibitor used as a cognitive enhancer in the treatment of Alzheimer"s disease (AD). tha 0-7 acetylcholinesterase Rattus norvegicus 36-40 22192081-6 2012 Additionally, tacrine was shown to be more efficient in brain AChE inhibition than T2 tacrine analogue and less active than T1 tacrine analogue, whereas BuChE inhibition followed the order: T1 > T2 > tacrine. tha 14-21 acetylcholinesterase Rattus norvegicus 62-66 21621296-3 2012 Treatment of SH-SY5Y cells with the AChE-inhibitor tacrine decreased PS1 levels, in parallel with increase in the secretion of amyloid precursor protein APPalpha, whereas the cholinergic agonist carbachol had no effect on PS1. tha 51-58 presenilin 1 Homo sapiens 69-72 21621296-6 2012 Mice administered with tacrine or donepezil displayed lower levels of brain PS1. tha 23-30 presenilin 1 Mus musculus 76-79 21994917-3 2011 The enzyme kinetics and the inhibition effects of three types of AChE inhibitors, which are tacrine, carbofuran and parathion-methyl, have been investigated using an amperometric method. tha 92-99 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-69 22032870-3 2012 The structure of tacrine, an acetylcholinesterase (AChE) inhibitor (AChEI), has been widely used as scaffold to provide new MTDLs. tha 17-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 29-49 22032870-3 2012 The structure of tacrine, an acetylcholinesterase (AChE) inhibitor (AChEI), has been widely used as scaffold to provide new MTDLs. tha 17-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-55 22032870-6 2012 In this study we demonstrated that the cystamine-tacrine dimer is endowed with a lower toxicity in comparison to bis(7)tacrine, it is able to inhibit AChE, butyrylcholinesterase (BChE), self- and AChE-induced beta-amyloid aggregation in the same range of the reference compound and exerts a neuroprotective action on SH-SY5Y cell line against H(2)O(2)-induced oxidative injury. tha 49-56 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-154 22032870-6 2012 In this study we demonstrated that the cystamine-tacrine dimer is endowed with a lower toxicity in comparison to bis(7)tacrine, it is able to inhibit AChE, butyrylcholinesterase (BChE), self- and AChE-induced beta-amyloid aggregation in the same range of the reference compound and exerts a neuroprotective action on SH-SY5Y cell line against H(2)O(2)-induced oxidative injury. tha 49-56 butyrylcholinesterase Homo sapiens 156-177 22032870-6 2012 In this study we demonstrated that the cystamine-tacrine dimer is endowed with a lower toxicity in comparison to bis(7)tacrine, it is able to inhibit AChE, butyrylcholinesterase (BChE), self- and AChE-induced beta-amyloid aggregation in the same range of the reference compound and exerts a neuroprotective action on SH-SY5Y cell line against H(2)O(2)-induced oxidative injury. tha 49-56 butyrylcholinesterase Homo sapiens 179-183 22032870-6 2012 In this study we demonstrated that the cystamine-tacrine dimer is endowed with a lower toxicity in comparison to bis(7)tacrine, it is able to inhibit AChE, butyrylcholinesterase (BChE), self- and AChE-induced beta-amyloid aggregation in the same range of the reference compound and exerts a neuroprotective action on SH-SY5Y cell line against H(2)O(2)-induced oxidative injury. tha 49-56 acetylcholinesterase (Cartwright blood group) Homo sapiens 196-200 22032870-7 2012 The investigation of the mechanism of neuroprotection showed that the cystamine-tacrine dimer acts by activating kinase 1 and 2 (ERK1/2) and Akt/protein kinase B (PKB) pathways. tha 80-87 mitogen-activated protein kinase 3 Homo sapiens 129-135 22032870-7 2012 The investigation of the mechanism of neuroprotection showed that the cystamine-tacrine dimer acts by activating kinase 1 and 2 (ERK1/2) and Akt/protein kinase B (PKB) pathways. tha 80-87 AKT serine/threonine kinase 1 Homo sapiens 141-144 22032870-7 2012 The investigation of the mechanism of neuroprotection showed that the cystamine-tacrine dimer acts by activating kinase 1 and 2 (ERK1/2) and Akt/protein kinase B (PKB) pathways. tha 80-87 AKT serine/threonine kinase 1 Homo sapiens 163-166 21620901-5 2011 Acetylcholinesterase inhibitors tacrine and donepezil (5mg/kg, PO) pretreatment significantly prevented STZ induced memory deficit, oxidative stress, Ca(2+) influx and caspase-3 activity. tha 32-39 acetylcholinesterase Rattus norvegicus 0-20 22949848-1 2012 In the present study we describe the synthesis and biological assessment of new tacrine analogs in the course of inhibition of acetylcholinesterase. tha 80-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-147 21620901-5 2011 Acetylcholinesterase inhibitors tacrine and donepezil (5mg/kg, PO) pretreatment significantly prevented STZ induced memory deficit, oxidative stress, Ca(2+) influx and caspase-3 activity. tha 32-39 caspase 3 Rattus norvegicus 168-177 21871694-0 2011 Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation inhibitors. tha 27-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 52-72 21472649-3 2011 In the acute assay, THA caused greater total cholesterol (37 %) and triglyceride (46 %) serum level reduction than lovastatin (32 and 1 %), a HMG-CoA reductase inhibitor or orlistat (26 and 34 %), a gastrointestinal lipase inhibitor. tha 20-23 lipase, endothelial Mus musculus 216-222 21570751-1 2011 The synthesis and biochemical evaluation of new hybrids of tacrine (THA) and 4-fluorobenzoic acid (4-FBA) possessing activity towards acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition are presented. tha 59-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-154 21621811-3 2011 The main class of medicines which are applied in AD is acetylcholinesterase inhibitors (AChEIs) like tacrine, donepezil, galantamine and rivastigmine that do not contribute to significant and long-term improvement in cognitive and behavioural functions. tha 101-108 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-75 21570751-1 2011 The synthesis and biochemical evaluation of new hybrids of tacrine (THA) and 4-fluorobenzoic acid (4-FBA) possessing activity towards acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition are presented. tha 68-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-154 21497158-1 2011 We have recently synthesized a new series of hybrid compounds having the moieties of tacrine, a potent inhibitor of brain and peripheral acetylcholinesterase (AChE), and nimodipine, a blocker of L-type voltage-dependent calcium channels (VDCCs). tha 85-92 acetylcholinesterase Rattus norvegicus 159-163 20981864-9 2011 Best in vivo protection from DFP-induced mortality was achieved when physostigmine (RR = 0.02) or tacrine (RR = 0.05) was given before DFP exposure, which was significantly superior to the pretreatment with all other tested compounds, except K-27 (RR = 0.18). tha 98-105 keratin 27 Rattus norvegicus 242-246 20981864-12 2011 K-27 may be a more efficacious alternative to pyridostigmine, when passage into the brain precludes administration of physostigmine or tacrine. tha 135-142 keratin 27 Rattus norvegicus 0-4 21553703-1 2011 Drugs currently approved by the U.S. Food and Drug Administration (FDA) for the treatment of Alzheimer"s disease include acetylcholinesterase inhibitor (i.e., tacrine, donepezil, rivastigmine, and galantamine) and glutamate-modulating (i.e., memantine) drugs. tha 159-166 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-141 21232021-2 2011 The aim of this study was to evaluate the effect of tacrine, an acetylcholinesterase inhibitor, on recognition memory as well as the associated hepatotoxicity in juvenile (20-day-old) and adult (100-day-old) ICR male mice. tha 52-59 acetylcholinesterase Mus musculus 64-84 21232021-10 2011 Tacrine 40 mumol/kg elevated the serum alanine aminotransferase (ALT) activity (by 135%) in juvenile mice, but reduced the ALT activity (by 42%) in adult mice. tha 0-7 glutamic pyruvic transaminase, soluble Mus musculus 39-63 21232021-10 2011 Tacrine 40 mumol/kg elevated the serum alanine aminotransferase (ALT) activity (by 135%) in juvenile mice, but reduced the ALT activity (by 42%) in adult mice. tha 0-7 glutamic pyruvic transaminase, soluble Mus musculus 65-68 21232021-10 2011 Tacrine 40 mumol/kg elevated the serum alanine aminotransferase (ALT) activity (by 135%) in juvenile mice, but reduced the ALT activity (by 42%) in adult mice. tha 0-7 glutamic pyruvic transaminase, soluble Mus musculus 123-126 21497959-1 2011 A new series of heterobivalent tacrine derivatives were designed, synthesized and evaluated as potential multi-functional anti-Alzheimer agents for their inhibitory activity on cholinesterases, antioxidant activity and self-induced beta-amyloid (Abeta) aggregation. tha 31-38 amyloid beta precursor protein Homo sapiens 246-251 21699076-6 2011 Compound 3e showed stronger activity than the standard tacrine, and compound 3a showed activity similar to that of tacrine for AChE. tha 115-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 21247200-2 2011 Using fast kinetic whole-cell recording, we have now studied effects of tacrine, an agent used clinically to treat Alzheimer"s disease, on currents elicited by activation of rat alpha(3)beta(4) nAChR heterologously expressed in KXalpha3beta4R2 cells. tha 72-79 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 194-199 21247200-4 2011 Experiments were performed to investigate whether tacrine is able to activate the alpha(3)beta(4) nAChR. tha 50-57 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 98-103 21247200-7 2011 The increase of Phi(-1) in the presence of tacrine suggests that the drug stabilizes a nonconducting open channel form of the receptor. tha 43-50 protein phosphatase 1, regulatory (inhibitor) subunit 14B Rattus norvegicus 16-22 21152577-0 2011 Clicked tacrine conjugates as acetylcholinesterase and beta-amyloid directed compounds. tha 8-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 21148081-0 2011 Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats. tha 87-94 butyrylcholinesterase Rattus norvegicus 50-64 21152577-1 2011 The multifaceted nature of Alzheimer"s disease (AD) has led to the development of multi-targeted compounds based on the classical AD drug, tacrine, first known to inhibit the acetylcholine-degrading enzyme acetylcholinesterase (AChE). tha 139-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 206-226 21152577-1 2011 The multifaceted nature of Alzheimer"s disease (AD) has led to the development of multi-targeted compounds based on the classical AD drug, tacrine, first known to inhibit the acetylcholine-degrading enzyme acetylcholinesterase (AChE). tha 139-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 228-232 21152577-6 2011 Moreover, they have the capacity to bind to Abeta(40) fibrils (SPR assays) while retaining the AChE inhibitory activity of the parent tacrine. tha 134-141 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 21116174-1 2011 Acetylcholinesterase inhibitors (AChE-Is), galantamine, physostigmine and tacrine, enhance central levels of synaptic acetylcholine. tha 74-81 acetylcholinesterase Rattus norvegicus 0-20 21343890-1 2011 A facile synthesis of potential acetylcholinesterase (AChE) inhibitors, the tacrine analogues 3a-p, has been accomplished by direct cyclocondensation of 1-aryl-4-cyano-5-aminopyrazole with beta-ketoesters using tin(IV) chloride as catalyst. tha 76-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-52 21343890-1 2011 A facile synthesis of potential acetylcholinesterase (AChE) inhibitors, the tacrine analogues 3a-p, has been accomplished by direct cyclocondensation of 1-aryl-4-cyano-5-aminopyrazole with beta-ketoesters using tin(IV) chloride as catalyst. tha 76-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 54-58 21211982-2 2011 All the synthesized compounds had high acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity with IC50 values at the nanomolar range, which were much better than tacrine alone. tha 190-197 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-59 21211982-2 2011 All the synthesized compounds had high acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity with IC50 values at the nanomolar range, which were much better than tacrine alone. tha 190-197 butyrylcholinesterase Homo sapiens 71-92 21127466-1 2010 A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. tha 6-13 butyrylcholinesterase Homo sapiens 20-34 22173266-1 2011 We recently observed that pretreatment with the cholinesterase inhibitor, tacrine can produce long-lasting reductions in cocaine-reinforced behavior, described as persistent attenuation. tha 74-81 butyrylcholinesterase Rattus norvegicus 48-62 21127466-1 2010 A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 190-242 21090615-3 2010 The click-chemistry inhibitor TZ2PA6 links the active center ligand, tacrine, to the peripheral site ligand, propidium, through a biorthogonal reaction of an acetylene and an azide that forms either a syn1 or an anti1 triazole. tha 69-76 synapsin I Mus musculus 201-205 21199749-4 2010 At present, there are five drugs approved in the United States for the treatment of AD, namely, donepezil, galantamine, rivastigmine, and tacrine (which are all cholinesterase inhibitors); and memantine (which is a glutamate receptor antagonist). tha 138-145 butyrylcholinesterase Homo sapiens 161-175 20466502-0 2010 Production and on-line acetylcholinesterase bioactivity profiling of chemical and biological degradation products of tacrine. tha 117-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 23-43 21567838-4 2010 Students carry out the computational modeling of the interaction of acetylcholinesterase and its inhibitor, tacrine, and learn about the concepts of protein structure, enzyme-inhibitor interactions, intermolecular forces, and role of molecular design in drug-development. tha 108-115 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-88 20545360-1 2010 Tacrine and PBT2 (an 8-hydroxyquinoline derivative) are well-known drugs that inhibit cholinesterases and decrease beta-amyloid (Abeta) levels by complexation of redox-active metals, respectively. tha 0-7 amyloid beta precursor protein Homo sapiens 129-134 21044529-0 2010 Changes in cytochrome oxidase activity following spatial working memory learning in rats treated with tacrine. tha 102-109 coproporphyrinogen oxidase Rattus norvegicus 11-29 21044529-1 2010 We evaluated change in cytochrome oxidase (COx) activity of the hippocampus and related structures of the limbic system following spatial working memory learning in rats after treatment with tacrine (8.0mg/kg). tha 191-198 coproporphyrinogen oxidase Rattus norvegicus 23-41 21044529-1 2010 We evaluated change in cytochrome oxidase (COx) activity of the hippocampus and related structures of the limbic system following spatial working memory learning in rats after treatment with tacrine (8.0mg/kg). tha 191-198 coproporphyrinogen oxidase Rattus norvegicus 43-46 21044529-4 2010 The tacrine and saline groups showed similar behavioral results, but a decrease in COx activity was found in the tacrine group in the prefrontal cortex, nucleus accumbens, anterior thalamus, hippocampus and nucleus basalis of Meynert. tha 113-120 coproporphyrinogen oxidase Rattus norvegicus 83-86 21044529-7 2010 The tacrine group presented the same increase in the anterodorsal thalamus, dentate gyrus, CA3 and mammillary nuclei. tha 4-11 carbonic anhydrase 3 Rattus norvegicus 91-94 19774434-3 2010 Tacrine and melatonin are well-known drugs which act as an acetylcholinesterase inhibitor and a free radical scavenger, respectively. tha 0-7 acetylcholinesterase Mus musculus 59-79 21483585-7 2010 Consistent with these observations, THA pre-treatment normalized the activities of antioxidant enzymes, such as catalase, glutathione peroxidase, and superoxide dismutase, and increased the levels of reduced glutathione (GSH) in CCl(4)-treated mice. tha 36-39 catalase Mus musculus 112-120 19961320-1 2010 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). tha 114-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 20006600-0 2010 Differential effects of systemic and intraseptal administration of the acetylcholinesterase inhibitor tacrine on the recovery of spatial behavior in an animal model of diencephalic amnesia. tha 102-109 acetylcholinesterase Rattus norvegicus 71-91 20043893-1 2010 Bis(7)-tacrine [bis(7)-tetrahydroaminacrine] is a dimeric AChE inhibitor derived from tacrine with a potential to treat Alzheimer"s disease. tha 7-14 acetylcholinesterase Rattus norvegicus 58-62 20205672-5 2010 These studies suggest that treatment with rapidly-reversible cholinesterase inhibitors (e.g. donepezil, galantamine, tacrine) are associated with marked and significant upregulation of AChE activities and protein levels in the CSF of AD patients. tha 117-124 butyrylcholinesterase Homo sapiens 61-75 20533758-0 2010 Tacrine-NO donor and tacrine-ferulic acid hybrid molecules as new anti-Alzheimer agents: hepatotoxicity and influence on the cytochrome P450 system in comparison to tacrine. tha 0-7 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 125-140 19944736-7 2010 In addition, tacrine-loaded nanoparticles administration induced damage of neuronal cells in CA1 field of the hippocampus in all treated animals, while the saline solution of tacrine only in 60% of animals. tha 13-20 carbonic anhydrase 1 Rattus norvegicus 93-96 20533758-6 2010 Tacrine caused pericentral necrosis and fatty degeneration of the hepatocytes, loss of liver glycogen and (indicating oxidative stress) induction of heme oxygenase (HO)-1. tha 0-7 heme oxygenase 1 Rattus norvegicus 149-170 20533758-8 2010 Both tacrine and the hybrids, but mainly FL38 and FL67, caused an induction of CYP1A1, 2B1 and 3A2 expression. tha 5-12 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 79-85 20533758-8 2010 Both tacrine and the hybrids, but mainly FL38 and FL67, caused an induction of CYP1A1, 2B1 and 3A2 expression. tha 5-12 UDP glucuronosyltransferase family 2 member B17 Rattus norvegicus 87-98 20345341-9 2010 This review will focus on and summarize the last two years of research into the development of tacrine derivatives able to hit AD targets beyond simple AChE inhibition. tha 95-102 acetylcholinesterase (Cartwright blood group) Homo sapiens 152-156 19736302-9 2009 Blockade of HCN2 currents by 100 microM 9-amino-1,2,3,4-tetrahydroacridine (THA) stopped spontaneous activity and subsequent washout restored it. tha 40-74 hyperpolarization activated cyclic nucleotide gated potassium and sodium channel 2 Homo sapiens 12-16 20648918-2 2010 In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). tha 18-25 acetylcholinesterase Rattus norvegicus 59-79 20648918-2 2010 In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). tha 18-25 acetylcholinesterase Rattus norvegicus 81-85 20648918-2 2010 In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). tha 18-25 butyrylcholinesterase Rattus norvegicus 122-143 20648918-2 2010 In vitro, the two tacrine-ferulic acid hybrids show higher acetylcholinesterase (AChE) inhibitory activity and comparable butyrylcholinesterase (BChE) inhibitory activity compared to tacrine (CAS 1684-40-8). tha 18-25 butyrylcholinesterase Rattus norvegicus 145-149 19714494-4 2010 Donepezil, galanatamine and tacrine, therapeutic acetylcholinesterase (AChE) inhibitors currently being used for treatment of Alzheimer"s disease also protected neuronal cells from glutamate neurotoxicity. tha 28-35 acetylcholinesterase Rattus norvegicus 49-69 19714494-4 2010 Donepezil, galanatamine and tacrine, therapeutic acetylcholinesterase (AChE) inhibitors currently being used for treatment of Alzheimer"s disease also protected neuronal cells from glutamate neurotoxicity. tha 28-35 acetylcholinesterase Rattus norvegicus 71-75 19932643-1 2009 A rapid simultaneous determination method for in vitro Cytochrome P450 (CYP) activity assay of 1,2,3,4-tetrahydroacridin-9-amine (tacrine) metabolites using ultra high performance liquid chromatography (UHPLC) coupled with computer-assisted in-source collision induced dissociation (CID) monitoring was investigated. tha 95-128 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 55-70 19932643-1 2009 A rapid simultaneous determination method for in vitro Cytochrome P450 (CYP) activity assay of 1,2,3,4-tetrahydroacridin-9-amine (tacrine) metabolites using ultra high performance liquid chromatography (UHPLC) coupled with computer-assisted in-source collision induced dissociation (CID) monitoring was investigated. tha 95-128 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 72-75 19932643-1 2009 A rapid simultaneous determination method for in vitro Cytochrome P450 (CYP) activity assay of 1,2,3,4-tetrahydroacridin-9-amine (tacrine) metabolites using ultra high performance liquid chromatography (UHPLC) coupled with computer-assisted in-source collision induced dissociation (CID) monitoring was investigated. tha 130-137 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 55-70 19932643-1 2009 A rapid simultaneous determination method for in vitro Cytochrome P450 (CYP) activity assay of 1,2,3,4-tetrahydroacridin-9-amine (tacrine) metabolites using ultra high performance liquid chromatography (UHPLC) coupled with computer-assisted in-source collision induced dissociation (CID) monitoring was investigated. tha 130-137 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 72-75 19695303-6 2009 The study becomes interesting because of i) the cobra venom AChE exists in monomeric globular forms; ii) in Alzheimer"s disease too the most abundant forms of cholinesterases are monomeric globular forms, thought to be involved in the pathogenesis of Alzheimer"s disease; iii) the effect of Alzheimer"s disease drugs on the AAA activity of cobra venom, indicated that AAA activity of cobra venom was more sensitive than AChE and iv) Huperzine and Tacrine showed more pronounced effect on AAA. tha 447-454 acetylcholinesterase Capra hircus 60-64 20648918-5 2010 The beta-carboline derivatives 2A, 2B, and 2 C, the inhibitory potency of which at AChE reaching tacrine activity does not antagonize scopolamine induced impairment of cognition in rats measured in radial maze paradigm. tha 97-104 acetylcholinesterase Rattus norvegicus 83-87 19736302-9 2009 Blockade of HCN2 currents by 100 microM 9-amino-1,2,3,4-tetrahydroacridine (THA) stopped spontaneous activity and subsequent washout restored it. tha 76-79 hyperpolarization activated cyclic nucleotide gated potassium and sodium channel 2 Homo sapiens 12-16 19374444-1 2009 Tacripyrines (1-14) have been designed by combining an AChE inhibitor (tacrine) with a calcium antagonist such as nimodipine and are targeted to develop a multitarget therapeutic strategy to confront AD. tha 71-78 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-59 19698738-0 2009 Long-lasting decreases in cocaine-reinforced behavior following treatment with the cholinesterase inhibitor tacrine in rats selectively bred for drug self-administration. tha 108-115 butyrylcholinesterase Rattus norvegicus 83-97 19698738-1 2009 Tacrine is a centrally acting, reversible cholinesterase inhibitor that increases synaptic levels of acetylcholine (ACh) and can potentiate the actions of dopamine (DA). tha 0-7 butyrylcholinesterase Rattus norvegicus 42-56 19698738-1 2009 Tacrine is a centrally acting, reversible cholinesterase inhibitor that increases synaptic levels of acetylcholine (ACh) and can potentiate the actions of dopamine (DA). tha 0-7 acyl-CoA thioesterase 12 Rattus norvegicus 82-120 19590965-1 2009 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a variety of clinically important drugs (e.g., clozapine, tacrine, tizanidine, and theophylline), a number of procarcinogens (e.g. benzo[a]pyrene and aflatoxin B(1)), and several important endogenous compounds (e.g. steroids and arachidonic acids). tha 127-134 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 19702529-1 2009 CYP1A2 is one of the major CYPs in human liver ( approximately 13%) and metabolises a variety of clinically important drugs, such as clozapine, lidocaine, theophylline, tacrine, and leflunomide. tha 169-176 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 0-6 19370562-3 2009 Tacrine, the first of the cholinesterase inhibitors to undergo extensive trials for this purpose, was associated with significant adverse effects including hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 26-40 19041670-4 2009 Tacrine is a reversible cholinesterase inhibitor used for treating mild to moderate AD. tha 0-7 butyrylcholinesterase Homo sapiens 24-38 19252271-2 2009 Donepezil, galantamine and tacrine are acetylcholinesterase inhibitors used for the treatment of Alzheimer"s disease, and were believed to be symptomatic drugs whose therapeutic effects are achieved by slowing the hydrolysis of acetylcholine at synaptic termini. tha 27-34 acetylcholinesterase Rattus norvegicus 39-59 19754423-5 2009 Typical CYP1A2 substrates generally contain planar ring that can fit the narrow and planar active site of the enzyme, such as propranolol, clozapine, guanabenz, flutamide, imatinib, thalidomide, carbamazepine, lidocaine, theophylline, tacrine, tizanidine, zolpidem, riluzole, zileuton, and leflunomide. tha 235-242 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 8-14 19110209-6 2009 Over the past decade, our group has developed several series of dimeric acetylcholinesterase (AChE) inhibitors derived from tacrine and huperzine A, a unique anti-Alzheimer"s drug originally discovered from a traditional Chinese medicinal plant. tha 124-131 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 19374459-3 2009 Two classes of medications have been approved by the US FDA for the treatment of Alzheimer"s disease: the cholinesterase inhibitors (tacrine, donepezil, rivastigmine, galantamine), mostly for mild to moderate Alzheimer"s disease, and the noncompetitive NMDA receptor antagonist memantine for the moderate to severe stages of Alzheimer"s disease. tha 133-140 butyrylcholinesterase Homo sapiens 106-120 19077124-10 2009 The AChE inhibitors tacrine and physostigmine enhanced control LTP. tha 20-27 acetylcholinesterase Rattus norvegicus 4-8 18693129-5 2009 Zonisamide suppressed the tacrine-induced c-Fos expression in the cortex, the dorsal striatum, and the nucleus accumbens, which are involved in the architecture of the cortico-basal ganglia-thalamocortical circuits. tha 26-33 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 42-47 19365154-8 2009 Tacrine and bis(7)-tacrine inhibited brain acetylcholinesterase (AChE) activity 15 min (but not 30 min) after the drug administration in mice. tha 0-7 acetylcholinesterase Mus musculus 43-63 19365154-8 2009 Tacrine and bis(7)-tacrine inhibited brain acetylcholinesterase (AChE) activity 15 min (but not 30 min) after the drug administration in mice. tha 0-7 acetylcholinesterase Mus musculus 65-69 19365154-9 2009 At the same dose of 20 micromol/kg, the bis(7)-tacrine-induced AChE inhibition in serum was 14-fold higher than that of tacrine. tha 47-54 acetylcholinesterase Mus musculus 63-67 19365154-11 2009 However, bis(7)-tacrine was more potent than tacrine in the cognitive enhancement of SCP-induced memory loss and in AChE inhibition. tha 16-23 acetylcholinesterase Mus musculus 116-120 18634893-3 2008 METHODS: The assay consisted of human liver microsomes and a cocktail of probe substrates metabolized by the five major CYP isoforms (tacrine for CYP1A2, diclofenac for CYP2C9, (S)-mephenytoin for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4). tha 134-141 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 120-123 18693129-0 2009 Effects of zonisamide on c-Fos expression under conditions of tacrine-induced tremulous jaw movements in rats: a potential mechanism underlying its anti-parkinsonian tremor effect. tha 62-69 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 25-30 19053746-1 2008 A series of tacrine-NO donor hybrid compounds are synthesized and evaluated for cholinesterase inhibitory activity, cognition improving activity, and hepatotoxicity. tha 12-19 butyrylcholinesterase Homo sapiens 80-94 19094390-7 2008 The inhibition effect of tacrine was calculated from the reaction-induced spectral changes, revealing an important decrease in the activity of AChE, approaching zero when the inhibitor concentration is high enough. tha 25-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 143-147 18634893-3 2008 METHODS: The assay consisted of human liver microsomes and a cocktail of probe substrates metabolized by the five major CYP isoforms (tacrine for CYP1A2, diclofenac for CYP2C9, (S)-mephenytoin for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4). tha 134-141 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 146-152 18555981-6 2008 In this communication we describe rationale for using purified recombinant Drosophila AChE as a template for in situ reaction of tacrine and propidium based libraries of acetylene and azide building blocks. tha 129-136 Acetylcholine esterase Drosophila melanogaster 86-90 18786825-1 2008 Tacrine based reversible inhibitors of cholinesterases (ChEIs) containing peptidic tethers were synthesized to interact with specific regions at the gorge level, and their potency was determined with human (h) acetylcholinesterase and butyrylcholinesterase. tha 0-7 butyrylcholinesterase Homo sapiens 235-256 18391858-10 2008 Tetrahydroaminoacridine administration after bilateral cervical vagotomy reversed hypotension and attenuated the plasma TNF-alpha response; in addition, it had no effect on the hepatic NF-kappaB activation. tha 0-23 tumor necrosis factor Rattus norvegicus 120-129 18577377-2 2008 The earliest known ChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of AD patients. tha 61-68 butyrylcholinesterase Homo sapiens 19-22 18573860-9 2008 In conclusion, tacrine, ethoxyresorufin, and phenacetin are probe substrates for CYP1A2 not only in humans but also in dogs. tha 15-22 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 81-87 18584988-3 2008 The 384-well assay used human liver microsomes in conjunction with a cocktail of probe substrates metabolized by the five major CYPs (tacrine for CYP1A2, diclofenac for CYP2C9, (S)-mephenytoin for CYP2C19, dextromethorphan for CYP2D6 and midazolam for CYP3A4). tha 134-141 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 146-152 18758020-1 2008 The title compound, C(14)H(14)ClN, is a chloro analogue of tacrine, an acetylcholinesterase inhibitor. tha 59-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-91 18640842-0 2008 New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. tha 4-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 49-69 19662147-1 2008 In this study we investigated the structure-activity relationships by using the Electron- Topological Method (ETM) for a class of AChE inhibitors related to tacrine (9-amino-1,2,3,4-tetrahydroacridine) and 11 H-Indeno-[1,2-b]-quinolin-10-ylamine that tetracyclic tacrine analogues, a drug currently in use for the treatment of the AD. tha 157-164 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 19662147-1 2008 In this study we investigated the structure-activity relationships by using the Electron- Topological Method (ETM) for a class of AChE inhibitors related to tacrine (9-amino-1,2,3,4-tetrahydroacridine) and 11 H-Indeno-[1,2-b]-quinolin-10-ylamine that tetracyclic tacrine analogues, a drug currently in use for the treatment of the AD. tha 166-200 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 19662147-1 2008 In this study we investigated the structure-activity relationships by using the Electron- Topological Method (ETM) for a class of AChE inhibitors related to tacrine (9-amino-1,2,3,4-tetrahydroacridine) and 11 H-Indeno-[1,2-b]-quinolin-10-ylamine that tetracyclic tacrine analogues, a drug currently in use for the treatment of the AD. tha 263-270 acetylcholinesterase (Cartwright blood group) Homo sapiens 130-134 18517184-1 2008 A novel series of donepezil-tacrine hybrids designed to simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-induced A beta aggregation. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-158 18517184-1 2008 A novel series of donepezil-tacrine hybrids designed to simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-induced A beta aggregation. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 18517184-1 2008 A novel series of donepezil-tacrine hybrids designed to simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-induced A beta aggregation. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 228-232 18517184-1 2008 A novel series of donepezil-tacrine hybrids designed to simultaneously interact with the active, peripheral and midgorge binding sites of acetylcholinesterase (AChE) have been synthesized and tested for their ability to inhibit AChE, butyrylcholinesterase (BChE), and AChE-induced A beta aggregation. tha 28-35 acetylcholinesterase (Cartwright blood group) Homo sapiens 228-232 18473751-2 2008 The formation of hydroxyderivatives of tacrine is well-established step in the metabolization of this drug in liver by microsomal cytochrome P450 enzymes family. tha 39-46 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 130-145 20641369-0 2004 [(111)In-Diethylenetriamine pentaacetic acid-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]bombesin(5-14) [(111)In-Diethylenetriamine pentaacetic acid-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]-bombesin(5-14) ([(111)In-DTPA-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]-BN(5-14)) is a peptide analog of the human gastrin-releasing peptide (GRP) conjugated with (111)In, and it was developed for single-photon emission computed tomography (SPECT) imaging of tumors with overexpressed GRP receptors (GRP-R) (1). tha 55-58 gastrin releasing peptide Homo sapiens 90-98 18316756-2 2008 PURPOSE: To review the evidence for the effectiveness of cholinesterase inhibitors (donepezil, galantamine, rivastigmine, and tacrine) and the neuropeptide-modifying agent memantine in achieving clinically relevant improvements, primarily in cognition, global function, behavior, and quality of life, for patients with dementia. tha 126-133 butyrylcholinesterase Homo sapiens 57-71 20641369-0 2004 [(111)In-Diethylenetriamine pentaacetic acid-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]bombesin(5-14) [(111)In-Diethylenetriamine pentaacetic acid-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]-bombesin(5-14) ([(111)In-DTPA-ACMpip(5),Tha(6),betaAla(11),Tha(13),NIe(14)]-BN(5-14)) is a peptide analog of the human gastrin-releasing peptide (GRP) conjugated with (111)In, and it was developed for single-photon emission computed tomography (SPECT) imaging of tumors with overexpressed GRP receptors (GRP-R) (1). tha 74-77 gastrin releasing peptide Homo sapiens 90-98 19453088-1 2008 The protective effect of the reversible cholinesterase inhibitors tacrine and pyridostigmine alone or in combination with different drugs against acetylcholinesterase inhibition in the pontomedullar area and cerebellum of rats caused by VX agent (O-ethyl S-2-diisopropylaminoethyl methyl phosphonothiolate) in vivo (2xLD50) was studied along with survival of animals pretreated with different combinations of the drugs used. tha 66-73 butyrylcholinesterase Rattus norvegicus 40-54 17917719-0 2008 Dose-related effects of the acetylcholinesterase inhibitor tacrine on cocaine and food self-administration in rats. tha 59-66 acetylcholinesterase Rattus norvegicus 28-48 23480140-3 2008 OBJECTIVE: This article reviews the development of novel classes of high affinity AChE inhibitors following a design strategy based on molecular hybridization by stepwise incorporation of different fragments of the known AChE inhibitors (-)-huperzine A and tacrine. tha 257-264 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 23480140-3 2008 OBJECTIVE: This article reviews the development of novel classes of high affinity AChE inhibitors following a design strategy based on molecular hybridization by stepwise incorporation of different fragments of the known AChE inhibitors (-)-huperzine A and tacrine. tha 257-264 acetylcholinesterase (Cartwright blood group) Homo sapiens 221-225 17917719-2 2008 Tacrine is a centrally acting, reversible cholinesterase inhibitor that also inhibits monoamine oxidase (MAO) and blocks reuptake of dopamine (DA) and serotonin. tha 0-7 butyrylcholinesterase Rattus norvegicus 42-56 17917719-2 2008 Tacrine is a centrally acting, reversible cholinesterase inhibitor that also inhibits monoamine oxidase (MAO) and blocks reuptake of dopamine (DA) and serotonin. tha 0-7 monoamine oxidase A Rattus norvegicus 86-103 17917719-2 2008 Tacrine is a centrally acting, reversible cholinesterase inhibitor that also inhibits monoamine oxidase (MAO) and blocks reuptake of dopamine (DA) and serotonin. tha 0-7 monoamine oxidase A Rattus norvegicus 105-108 17996678-6 2007 In contrast, tacrine was found to decrease ROS production (57% up to 102%) and TNFalpha level (up to 30%). tha 13-20 tumor necrosis factor Mus musculus 79-87 17996678-9 2007 Differential effects between PMS777 and tacrine could be attributed to the anti-PAF activity of PMS777 which was able to fight inflammatory events and oxidative injury whereas tacrine only minimizes them. tha 40-47 patchy fur Mus musculus 80-83 17944454-1 2007 Gallamine and tacrine are allosteric antagonists at muscarinic M2 acetylcholine receptors and inhibitors of acetylcholinesterase. tha 14-21 acetylcholinesterase (Cartwright blood group) Homo sapiens 108-128 17944454-2 2007 At both acetylcholine-binding proteins, gallamine and tacrine are known to occupy two different binding sites: in M2 receptors within the allosteric binding area and in acetylcholinesterase at its catalytic and its peripheral site. tha 54-61 acetylcholinesterase (Cartwright blood group) Homo sapiens 169-189 17848422-1 2007 BACKGROUND: There are 4 centrally acting cholinesterase inhibitors (CA-ChEI) available in the US: tacrine, galantamine, rivastigmine, and donepezil. tha 98-105 butyrylcholinesterase Homo sapiens 41-55 17823102-5 2007 The primary pharmacokinetic interactions with smoking occur with drugs that are CYP1A2 substrates, such as caffeine, clozapine, fluvoxamine, olanzapine, tacrine, and theophylline. tha 153-160 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 80-86 17883890-1 2007 In the treatment of Alzheimer"s disease tacrine, a cholinesterase inhibitor, is not the drug of choice due to its low oral bioavailability, extensive hepatic first-pass effect, rapid clearance from the systemic circulation, pronounced hepatotoxicity, and the availability of drugs better than tacrine in the same pharmacological class. tha 40-47 butyrylcholinesterase Mus musculus 51-65 17908053-5 2007 Some cholinesterase inhibitors (tacrine, donepezil, galantamine) are metabolized via CYP-related enzymes, especially CYP2D6, CYP3A4, and CYP1A2. tha 32-39 butyrylcholinesterase Homo sapiens 5-19 17908053-5 2007 Some cholinesterase inhibitors (tacrine, donepezil, galantamine) are metabolized via CYP-related enzymes, especially CYP2D6, CYP3A4, and CYP1A2. tha 32-39 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 117-123 17908053-5 2007 Some cholinesterase inhibitors (tacrine, donepezil, galantamine) are metabolized via CYP-related enzymes, especially CYP2D6, CYP3A4, and CYP1A2. tha 32-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 17908053-5 2007 Some cholinesterase inhibitors (tacrine, donepezil, galantamine) are metabolized via CYP-related enzymes, especially CYP2D6, CYP3A4, and CYP1A2. tha 32-39 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 137-143 17395211-5 2007 It was found that administration of tacrine, rivastigmine and donepezil in mice significantly attenuated the LPS induced increased levels of IL-2 along with the significant reduction of AChE activity predominantly in salt soluble (SS) fraction as compared to the detergent soluble (DS) fraction in a dose dependent manner. tha 36-43 interleukin 2 Mus musculus 141-145 18075466-0 2007 Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity. tha 54-61 interleukin 6 Homo sapiens 37-50 18075466-1 2007 BACKGROUND: Tacrine, an anticholinesterase used to treat Alzheimer"s disease (AD), leads to an increase in serum alanine aminotransferase (ALT) levels. tha 12-19 glutamic--pyruvic transaminase Homo sapiens 113-137 18075466-6 2007 On the basis of the gene expression data, the IL6 gene was identified as a potential candidate for tacrine transaminitis susceptibility. tha 99-106 interleukin 6 Rattus norvegicus 46-49 18075466-13 2007 CONCLUSION: The IL6 genotype may act as a predisposing factor for tacrine transaminitis. tha 66-73 interleukin 6 Homo sapiens 16-19 17363469-5 2007 To further define the mechanism, the effect of THA on the excretion of sulfobromophthalein (BSP) and disulfobromophthalein (DBSP), typical multidrug resistance protein-2 (Mrp2) substrates was examined. tha 47-50 ATP binding cassette subfamily B member 4 Rattus norvegicus 139-169 17395211-5 2007 It was found that administration of tacrine, rivastigmine and donepezil in mice significantly attenuated the LPS induced increased levels of IL-2 along with the significant reduction of AChE activity predominantly in salt soluble (SS) fraction as compared to the detergent soluble (DS) fraction in a dose dependent manner. tha 36-43 acetylcholinesterase Mus musculus 186-190 17389249-6 2007 Furthermore, the D439N mutation converted l-glutamate, THA, and PDC, which are activating substrates for the wild-type anion conductance, but not l-aspartate, into transient inhibitors of the EAAC1(D439) anion conductance. tha 55-58 solute carrier family 1 member 1 Homo sapiens 192-197 17158047-0 2007 Quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity using variable selections. tha 55-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-103 17363469-7 2007 Because DBSP is excreted without conjugation to glutathione, in contrast to BSP, the findings suggest that THA might compete with DBSP and BSP metabolites at a common canalicular transport site, presumably Mrp2. tha 107-110 ATP binding cassette subfamily B member 4 Rattus norvegicus 206-210 17363469-10 2007 THA also partially reversed the cholestatic effects of estradiol-17beta-D-glucuronide, a process also dependent on Mrp2. tha 0-3 ATP binding cassette subfamily B member 4 Rattus norvegicus 115-119 17363469-11 2007 In conclusion, the choleretic activity of THA and its possible metabolites is dependent on Mrp2. tha 42-45 ATP binding cassette subfamily B member 4 Rattus norvegicus 91-95 17158047-0 2007 Quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity using variable selections. tha 55-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 17158047-1 2007 A diverse approach to the quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity was studied using variable selections of stepwise multiple linear regression (MLR), genetic algorithm (GA)-MLR, and simulated annealing (SA)-MLR. tha 81-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 109-129 17158047-1 2007 A diverse approach to the quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity was studied using variable selections of stepwise multiple linear regression (MLR), genetic algorithm (GA)-MLR, and simulated annealing (SA)-MLR. tha 81-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-135 17158047-2 2007 AChE activity (logRA) of tacrine derivatives was expressed with acceptable explanation (95.5-95.9%) and good predictive power (94.5-95.2%), respectively, in the models. tha 25-32 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 17166674-1 2007 Controversial results about the involvement of CYP 1A2 and oxidative stress in tacrine-induced hepatotoxicity have been described by the different research groups. tha 79-86 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 47-54 16568139-11 2007 Western blot analysis showed a significantly higher level of TNF-alpha in C than in THA and THB at 1.5 h of reperfusion, but no difference was observed between C, THA, or THB at 3 or 5 days of reperfusion. tha 84-87 tumor necrosis factor Oryctolagus cuniculus 61-70 17166674-6 2007 The fact that fluvoxamine, a potent cytochrome P450 (CYP) 1A2 inhibitor, reduced tacrine toxicity and the expression of the CYP 1A2 gene was maintained in gel entrapped hepatocytes, but not in hepatocyte monolayers, could illustrate a close association between CYP 1A2 expression levels and tacrine toxicity. tha 291-298 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 124-131 17174470-2 2007 It has been reported previously that tacrine and some other AChE inhibitors suppressed I(K(A)) in central and peripheral neurons. tha 37-44 acetylcholinesterase Rattus norvegicus 60-64 17252937-0 2006 Modeling of acetylcholinesterase inhibition by tacrine analogues using Bayesian-regularized Genetic Neural Networks and ensemble averaging. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 12-32 17181144-0 2006 Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer"s disease. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-84 17181144-2 2006 These multipotent molecules are the result of the juxtaposition of an acetylcholinesterase inhibitor (AChEI) such as tacrine (1) and a 1,4-DHP such as nimodipine (2). tha 117-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-90 17252937-1 2006 Acetylcholinesterase inhibition was modeled for a set of 136 tacrine analogues using Bayesian-regularized Genetic Neural Networks (BRGNNs). tha 61-68 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 17415482-1 2006 The fluorescence intensity of reversible inhibitor ethidium bromide fluorophore complex with equine blood butyryl cholinesterase decreases in the presence of inhibitor (tacrine) not fluorescing in the visible spectrum. tha 169-176 butyrylcholinesterase Equus caballus 114-128 16413803-6 2006 In this work we proposed molecular hybrids of tacrine with donepezil (fusion of these structures), in order to suggest new proposals of AChE inhibitors for future treatment of AD. tha 46-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 136-140 17034128-0 2006 In-situ synthesis of a tacrine-triazole-based inhibitor of acetylcholinesterase: configurational selection imposed by steric interactions. tha 23-30 acetylcholinesterase (Cartwright blood group) Homo sapiens 59-79 17062329-9 2006 Two double-label and open-label clinical studies suggested that there may be a 3-way interaction between apolipoprotein E genotype, sex, and tacrine (range, P = 0.03 to P = 0.05). tha 141-148 apolipoprotein E Homo sapiens 105-121 16762377-1 2006 We show here that donepezil, galanathamine and tacrine, therapeutic acetylcholinesterase inhibitors currently being used for treatment of Alzheimer"s disease, protect neuronal cells in a time- and concentration-dependent manner from glutamate neurotoxicity that involves apoptosis. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-88 16643965-2 2006 Acute injection of 5-HT(1A) agonists 8-OH-DPAT and buspirone dose-dependently counteracted the tacrine-induced oral movements (ED(50)=0.04 and 1.0mg/kg, respectively), an effect reversed by the selective 5-HT(1A) antagonist WAY 100,635. tha 95-102 5-hydroxytryptamine receptor 1A Rattus norvegicus 19-26 16880719-1 2006 Donepezil, galanthamine, and tacrine are therapeutic acetylcholinesterase (AChE) inhibitors used for the treatment of Alzheimer"s disease. tha 29-36 acetylcholinesterase Rattus norvegicus 53-73 16880719-1 2006 Donepezil, galanthamine, and tacrine are therapeutic acetylcholinesterase (AChE) inhibitors used for the treatment of Alzheimer"s disease. tha 29-36 acetylcholinesterase Rattus norvegicus 75-79 16643965-2 2006 Acute injection of 5-HT(1A) agonists 8-OH-DPAT and buspirone dose-dependently counteracted the tacrine-induced oral movements (ED(50)=0.04 and 1.0mg/kg, respectively), an effect reversed by the selective 5-HT(1A) antagonist WAY 100,635. tha 95-102 5-hydroxytryptamine receptor 1A Rattus norvegicus 204-211 16643965-8 2006 These results show that 5-HT(1A) receptors play a role in the regulation of tacrine-induced TJM and suggest that their activation by novel antipsychotics may not only reduce the extrapyramidal side effects EPS liability, but also be effective in the treatment of parkinsonian tremor. tha 76-83 5-hydroxytryptamine receptor 1A Rattus norvegicus 24-31 16649535-0 2006 New tacrine-hydrazinonicotinamide hybrids as acetylcholinesterase inhibitors of potential interest for the early diagnostics of Alzheimer"s disease. tha 4-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-65 16599255-1 2006 Novel highly affine histamine H3 receptor ligands with additional inhibitory effects on the main histamine metabolizing enzyme in the brain, N-methyltransferase, chemically show structural elements of the acetylcholinesterase inhibitor tacrine. tha 236-243 histamine receptor H3 Homo sapiens 20-41 16420031-0 2006 Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-110 16420031-1 2006 Tacrine and melatonin are well-known drugs with activities as an acetylcholinesterase (AChE) inhibitor and free radical scavenger, respectively. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-85 16420031-1 2006 Tacrine and melatonin are well-known drugs with activities as an acetylcholinesterase (AChE) inhibitor and free radical scavenger, respectively. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 87-91 21162240-2 2006 METHODS: Melatonin and other drugs (Tacrine or DNQX) were microinjected into the CA3 area. tha 36-43 carbonic anhydrase 3 Rattus norvegicus 81-84 21162240-6 2006 (2) Melatonin could attenuate the excitation effect of Tacrine (inhibitor of AChE) on LTP. tha 55-62 acetylcholinesterase Rattus norvegicus 77-81 16649535-1 2006 The syntheses and the preliminary results of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by an affinity series of tacrine-hydrazinonicotinamide hybrids are described. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 45-65 16649535-1 2006 The syntheses and the preliminary results of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by an affinity series of tacrine-hydrazinonicotinamide hybrids are described. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 16649535-1 2006 The syntheses and the preliminary results of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by an affinity series of tacrine-hydrazinonicotinamide hybrids are described. tha 142-149 butyrylcholinesterase Homo sapiens 77-98 16649535-1 2006 The syntheses and the preliminary results of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by an affinity series of tacrine-hydrazinonicotinamide hybrids are described. tha 142-149 butyrylcholinesterase Homo sapiens 100-104 16649535-3 2006 Derivatives 6a and 6b showed lower activity than the model tacrine, while compounds 6c and 6d showed the strongest affinity to AChE. tha 59-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 127-131 16823990-9 2006 Nevertheless, because of their favourable pharmacological profile and bioavailability, the cholinesterase inhibitors tacrine and rivastigmine are expected to show at least the same benefits as oral formulations of these drugs, but with fewer severe adverse effects. tha 117-124 butyrylcholinesterase Homo sapiens 91-105 16373816-4 2006 Emergency physicians should strongly consider cholinesterase inhibitor (rivastigmine, galantamine, and tacrine) ingestion in patients who present with short and temporary organophosphate-like toxidromes. tha 103-110 butyrylcholinesterase Homo sapiens 46-60 17668702-0 2006 Effect of tacrine on cytosolic Ca2+ level and calmodulin in gastric muscle tissues of rat. tha 10-17 calmodulin 1 Rattus norvegicus 46-56 17668702-1 2006 INTRODUCTION: Tacrine is an acetylcholinesterase inhibitor. tha 14-21 acetylcholinesterase Rattus norvegicus 28-48 17668702-7 2006 AIM: The aim of this study was to investigate if tacrine induces reduction of calcium ions through chelation and/or inhibits directly calmodulin"s participation in the contractile processes, thus causing smooth muscle relaxation which is not characteristic of a typical acetylcholinesterase blocker. tha 49-56 calmodulin 1 Rattus norvegicus 134-144 17668702-7 2006 AIM: The aim of this study was to investigate if tacrine induces reduction of calcium ions through chelation and/or inhibits directly calmodulin"s participation in the contractile processes, thus causing smooth muscle relaxation which is not characteristic of a typical acetylcholinesterase blocker. tha 49-56 acetylcholinesterase Rattus norvegicus 270-290 17668702-13 2006 In the presence of trifluoperazine (a calmodulin blocker) 1 x 10(-4) mol/l tacrine causes relaxation which is commensurable with that in the controls. tha 75-82 calmodulin 1 Rattus norvegicus 38-48 17668702-14 2006 CONCLUSIONS: Tacrine-induced smooth muscle relaxation is not a result of the reduction of the effective Ca2+ concentrations as a result of chelation between tacrine and Ca2+ and it is not related to the tacrine effects on calmodulin. tha 13-20 calmodulin 1 Rattus norvegicus 222-232 19219825-1 2006 We sought to determine whether a non-originating surgeon early in his experience with the MIS two-incision technique for THA could place components with appropriate accuracy. tha 121-124 anti-Mullerian hormone Homo sapiens 90-93 16954599-5 2006 Oral administration of PPE or tacrine caused a dose-dependent inhibition of brain and plasma cholinesterase activities. tha 30-37 butyrylcholinesterase Rattus norvegicus 93-107 16309991-4 2005 Postoperative complications were observed in 4 hips of THA after TRO. tha 55-58 trophinin Homo sapiens 65-68 16183853-4 2005 Previous studies have identified several allosteric muscarinic ligands, including the acetylcholinesterase inhibitor tacrine and the bis-pyridinium derivative 4,4"-bis-[(2,6-dichloro-benzyloxy-imino)-methyl]-1,1"-propane-1,3-diyl-bis-pyridinium dibromide (Duo3), which, in contrast to conventional allosteric muscarinic ligands, display concentration-effect curves with slope factors >1. tha 117-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 86-106 15990178-1 2005 Tacrine is a potent and reversible inhibitor of acetylcholinesterase (AChE) in the brain. tha 0-7 acetylcholinesterase Mus musculus 70-74 15990178-6 2005 While in vivo inhibition of striatal AChE activity was observed only for the highest dose of tacrine, a dose-dependent increase in striatal choline acetyltransferase activity was obtained. tha 93-100 acetylcholinesterase Mus musculus 37-41 16128905-1 2005 The cytochrome P450 enzyme CYP1A2 mediates the rate-limiting step in the metabolism of many drugs including theophylline, clozapine, and tacrine as well as in the bioactivation of procarcinogens. tha 137-144 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 16230018-0 2005 Donepezil-tacrine hybrid related derivatives as new dual binding site inhibitors of AChE. tha 10-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-88 16168438-3 2005 The histamine receptor H1 antagonist diphenhydramine, the antimalarial drug amodiaquine, the antifolate drug metoprine, and the anticholinesterase drug tacrine (an early drug for Alzheimer"s disease) are surprisingly all potent HNMT inhibitors, having inhibition constants in the range of 10-100nM. tha 152-159 histamine N-methyltransferase Homo sapiens 228-232 16076210-1 2005 Recently, alkylene-linked heterodimers of tacrine (1) and 5-amino-5,6,7,8-tetrahydroquinolinone (2, hupyridone) were shown to exhibit higher acetylcholinesterase (AChE) inhibition than either monomeric 1 or 2. tha 42-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 141-161 16076210-1 2005 Recently, alkylene-linked heterodimers of tacrine (1) and 5-amino-5,6,7,8-tetrahydroquinolinone (2, hupyridone) were shown to exhibit higher acetylcholinesterase (AChE) inhibition than either monomeric 1 or 2. tha 42-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 163-167 15991031-2 2005 This study applied focal transcranial magnetic stimulation (TMS) to eight healthy subjects to test the effects of a single oral dose of 40 mg tacrine, an acetylcholinesterase inhibitor, on motor cortical excitability. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 154-174 15674800-0 2005 Synthesis and biological evaluation of tacrine-thiadiazolidinone hybrids as dual acetylcholinesterase inhibitors. tha 39-46 acetylcholinesterase (Cartwright blood group) Homo sapiens 81-101 15547049-8 2005 To determine whether OCT2 and/or OCTN2 transport tacrine, these transporters were cloned and then transfected in SK-HEP1 and HEK 293 cells. tha 49-56 solute carrier family 22 member 5 Homo sapiens 33-38 15547049-9 2005 The uptake of choline, MPP, and TEA was inhibited by the presence of tacrine in rOCT2-expressing SK-HEP1 cells, whereas the uptake of carnitine was inhibited by the presence of tacrine in rOCTN2-expressing HEK 293 cells. tha 69-76 solute carrier family 22 member 2 Rattus norvegicus 80-85 15670925-0 2005 Synthesis, acetylcholinesterase inhibition and neuroprotective activity of new tacrine analogues. tha 79-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 11-31 15852394-2 2005 We report that peripheral administration of the acetylcholinesterase inhibitors tacrine, rivastigmine, neostigmine, or EN101 (an antisense oligonucleotide directed at acetylcholinesterase messenger RNA) to mice significantly attenuated the production of interleukin-1beta in the hippocampus and blood, concomitantly with the reduction in acetylcholinesterase activity. tha 80-87 acetylcholinesterase Mus musculus 48-68 15882896-1 2005 In the present study, activity of salt soluble (SS) G1 and detergent soluble (DS) G4 molecular isoforms of acetylcholinesterase (AChE) has been investigated in rat brain areas in trained (learned), scopolamine (amnesic) and Tacrine (anti-dementic) treated rats to find out their role in learning and memory functions. tha 224-231 acetylcholinesterase Rattus norvegicus 107-127 15882896-5 2005 AChE activity was altered in both the fractions SS and DS of different brain areas following passive avoidance in control, scopolamine treated, tacrine treated and tacrine treatment in scopolamine pretreated rats. tha 144-151 acetylcholinesterase Rattus norvegicus 0-4 15882896-5 2005 AChE activity was altered in both the fractions SS and DS of different brain areas following passive avoidance in control, scopolamine treated, tacrine treated and tacrine treatment in scopolamine pretreated rats. tha 164-171 acetylcholinesterase Rattus norvegicus 0-4 15882896-9 2005 In hippocampus, AChE activity in the fraction G1 isoform (fraction 13 of SS) was decreased only in tacrine treated rats but AChE activity in the G4 isoform (fraction 9 of DS) was decreased in both trained and tacrine treated rats. tha 99-106 acetylcholinesterase Rattus norvegicus 16-20 15882896-10 2005 Changes in activity of G4 isoform of AChE in hippocampus could be correlated with passive avoidance learning, scopolamine induced deficit in passive avoidance and reversal of scopolamine deficit by tacrine. tha 198-205 acetylcholinesterase Rattus norvegicus 37-41 15834447-0 2005 Actions of tacrine and galanthamine on histamine-N-methyltransferase. tha 11-18 histamine N-methyltransferase Homo sapiens 39-68 15834447-2 2005 The AD medication tacrine was previously shown to inhibit some forms of rodent histamine-N-methyltransferase (HNMT), but the effects of AD drugs have not been investigated on human HNMT activity. tha 18-25 histamine N-methyltransferase Homo sapiens 79-108 15834447-2 2005 The AD medication tacrine was previously shown to inhibit some forms of rodent histamine-N-methyltransferase (HNMT), but the effects of AD drugs have not been investigated on human HNMT activity. tha 18-25 histamine N-methyltransferase Homo sapiens 110-114 15834447-3 2005 Presently, the effects of tacrine and galanthamine (another AD medication) were studied on the activity of several forms of human and rat HNMT. tha 26-33 histamine N-methyltransferase Rattus norvegicus 138-142 15834447-4 2005 Tacrine (0.01-10 microM) inhibited both human and rat HNMT activity in a concentration-dependent manner, but was less potent on both human embryonic kidney and recombinant human brain HNMT than on rat kidney HNMT (IC50 values were 0.46 and 0.70 microM vs. 0.29 microM, respectively). tha 0-7 histamine N-methyltransferase Rattus norvegicus 54-58 15834447-4 2005 Tacrine (0.01-10 microM) inhibited both human and rat HNMT activity in a concentration-dependent manner, but was less potent on both human embryonic kidney and recombinant human brain HNMT than on rat kidney HNMT (IC50 values were 0.46 and 0.70 microM vs. 0.29 microM, respectively). tha 0-7 histamine N-methyltransferase Homo sapiens 184-188 15834447-4 2005 Tacrine (0.01-10 microM) inhibited both human and rat HNMT activity in a concentration-dependent manner, but was less potent on both human embryonic kidney and recombinant human brain HNMT than on rat kidney HNMT (IC50 values were 0.46 and 0.70 microM vs. 0.29 microM, respectively). tha 0-7 histamine N-methyltransferase Rattus norvegicus 184-188 16544849-1 2005 INTRODUCTION: Tacrine is a cholinesterase inhibitor used for the treatment of Alzheimer"s disease. tha 14-21 butyrylcholinesterase Rattus norvegicus 27-41 15636707-12 2005 Tetrahydroamino-acridine (THA,1.5 mg/kg, intravenous drip administration after bilateral cervical vagotomy reversed hypotension and attenuated serum TNF-alpha and liver NF-KappaB amounts, but alpha-bungarotoxin (1.0 microg/kg intravenous drip) pretreatment reverted the inhibitory effects of vagal stimulation. tha 0-24 tumor necrosis factor Rattus norvegicus 149-158 15636707-12 2005 Tetrahydroamino-acridine (THA,1.5 mg/kg, intravenous drip administration after bilateral cervical vagotomy reversed hypotension and attenuated serum TNF-alpha and liver NF-KappaB amounts, but alpha-bungarotoxin (1.0 microg/kg intravenous drip) pretreatment reverted the inhibitory effects of vagal stimulation. tha 26-29 tumor necrosis factor Rattus norvegicus 149-158 15496314-2 2004 Other acetylcholinesterase inhibitors also increased the twitches, showing a hierarchy of potencies of galantamine>physostigmine>tacrine>rivastigmine=donepezil. tha 135-142 acetylcholinesterase Rattus norvegicus 6-26 16640027-3 2005 The influence of the THA (tacrine; 9-amino-1,2,3,4-tetrahydroacridine) on AChE inhibition by these substances was also evaluated. tha 26-33 acetylcholinesterase Rattus norvegicus 74-78 16640027-3 2005 The influence of the THA (tacrine; 9-amino-1,2,3,4-tetrahydroacridine) on AChE inhibition by these substances was also evaluated. tha 35-69 acetylcholinesterase Rattus norvegicus 74-78 15296848-1 2004 Acute administration of the acetylcholinesterase inhibitor tacrine to rats induces tremulous jaw movements which can be used as a valuable model of parkinsonian tremor. tha 59-66 acetylcholinesterase Rattus norvegicus 28-48 15469276-5 2004 In addition to the previously reported in situ product syn-TZ2PA6, we discovered three new inhibitors, syn-TZ2PA5, syn-TA2PZ6, and syn-TA2PZ5, derived from tacrine and phenylphenanthridinium azides and acetylenes, in the reactions with Electrophorus electricus and mouse AChE. tha 156-163 acetylcholinesterase Mus musculus 271-275 15258105-1 2004 Tacrine, a cholinesterase inhibitor, was approved for the treatment of Alzheimer"s disease. tha 0-7 butyrylcholinesterase Rattus norvegicus 11-25 15258105-6 2004 Preincubation of CYP1A2 with tacrine and NADPH revealed a time-dependent inhibition of 7-ethoxyresorufin O-de-ethylation with a K(i) of 1.94 microM and a k(inact) of 0.091 min(-1). tha 29-36 cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus 17-23 15246845-6 2004 Tetrahydroaminoacridine was a better reversible inhibitor of BuChE. tha 0-23 butyrylcholinesterase Homo sapiens 61-66 15304241-1 2004 The therapeutic approach for improving the cognitive function in patients with Alzheimer"s disease (AD) is mainly based on the potentiation of central cholinergic activity and is achieved clinically by the use of acetylcholinesterase (AChE) inhibitors such as tacrine, donepezil, rivastigmine, galantamine and other drugs currently in clinical trials. tha 260-267 acetylcholinesterase (Cartwright blood group) Homo sapiens 213-233 15304241-1 2004 The therapeutic approach for improving the cognitive function in patients with Alzheimer"s disease (AD) is mainly based on the potentiation of central cholinergic activity and is achieved clinically by the use of acetylcholinesterase (AChE) inhibitors such as tacrine, donepezil, rivastigmine, galantamine and other drugs currently in clinical trials. tha 260-267 acetylcholinesterase (Cartwright blood group) Homo sapiens 235-239 15350833-9 2004 The above-mentioned neuroprotective effects are also observed with tacrine (THA, 1 microM), suggesting that the neuroprotective effects of cholinesterase inhibitor might partly contribute to the clinical efficacy in AD treatment. tha 67-74 butyrylcholinesterase Rattus norvegicus 139-153 15350833-9 2004 The above-mentioned neuroprotective effects are also observed with tacrine (THA, 1 microM), suggesting that the neuroprotective effects of cholinesterase inhibitor might partly contribute to the clinical efficacy in AD treatment. tha 76-79 butyrylcholinesterase Rattus norvegicus 139-153 15265646-2 2004 In this study the model has been utilised to determine the effect of the acetylcholinesterase inhibiting compounds tacrine and physostigmine on spatial working memory deficits associated with the OB rat. tha 115-122 acetylcholinesterase Rattus norvegicus 73-93 15307384-8 2004 The results suggest, that in patients following THA with the elevated level of IL-6, the inflammatory process was present. tha 48-51 interleukin 6 Homo sapiens 79-83 15159498-1 2004 In this retrospective analysis of 443 Alzheimer disease (AD) patients from a 30-week tacrine trial, change in Alzheimer"s Disease Assessment Scale score from baseline to final value was significantly associated with a total serum cholesterol/APOE genotype interaction. tha 85-92 apolipoprotein E Homo sapiens 242-246 15131977-1 2004 We studied fluorescence of 9-amino-1,2,3,4-tetrahydroacridine hydrochloride (tacrine) in the presence of serum cholinesterase. tha 77-84 butyrylcholinesterase Homo sapiens 111-125 15131977-3 2004 A quenching mechanism is proposed; it includes formation of a complex and charge transfer mediated by excited tacrine molecule as well as indole of tryptophan residue from the periphery of cholinesterase active site. tha 110-117 butyrylcholinesterase Homo sapiens 189-203 15071608-1 2004 The clinical usage of the cholinesterase inhibitor tacrine for treatment of Alzheimer"s disease is accompanied by adverse effects on the gastrointestinal tract. tha 51-58 butyrylcholinesterase Rattus norvegicus 26-40 15106259-3 2004 Tacrine, the first of the cholinesterase inhibitors to undergo extensive trials for this purpose, was associated with significant adverse effects including hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 26-40 14754384-11 2004 Tacrine, the first acetylcholinesterase inhibitor who became available in 1993 as a treatment for AD, does not play an essential role anymore besides his historical value, because of its hepatotoxicity. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-39 15544502-3 2004 Effectiveness in AChE inhibition and side-effect issues of clinical (tacrine, donepezil, galanthamine and rivastigmine) as well as of novel inhibitors is reviewed here. tha 69-76 acetylcholinesterase (Cartwright blood group) Homo sapiens 17-21 15544507-2 2004 Thus, it is not surprising that the first therapeutic target that has demonstrated therapeutic efficacy on cognition, behaviour and functional daily activities has been the inhibitors of acetylcholinesterase (AChE), i.e. tacrine, donepezil, rivastigmine and galanthamine. tha 221-228 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-207 15544507-2 2004 Thus, it is not surprising that the first therapeutic target that has demonstrated therapeutic efficacy on cognition, behaviour and functional daily activities has been the inhibitors of acetylcholinesterase (AChE), i.e. tacrine, donepezil, rivastigmine and galanthamine. tha 221-228 acetylcholinesterase (Cartwright blood group) Homo sapiens 209-213 15544507-6 2004 In this frame, we have been synthesizing new tacrine derivatives that keep their ability to inhibit AChE but that interfere with neuronal calcium overloading and prevent apoptosis. tha 45-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-104 15211076-1 2004 Fifty consecutive outpatients with Alzheimer"s disease (AD) received treatment with the cholinesterase inhibitor tacrine in an open longitudinal study. tha 113-120 butyrylcholinesterase Homo sapiens 88-102 15132713-13 2004 Certainly, as a class, the currently approved cholinesterase inhibitors (donepezil, galantamine, rivastigmine and tacrine) provide important benefits in patients with Alzheimer"s disease and these drugs offer a significant advance in the management of dementia. tha 114-121 butyrylcholinesterase Homo sapiens 46-60 14681337-6 2004 Other classes of drugs that demonstrated inhibition of aldehyde oxidase included phenothiazines, tricyclic antidepressants, tricyclic atypical antipsychotic agents, and dihydropyridine calcium channel blockers, along with some other drugs, including loratadine, cyclobenzaprine, amodiaquine, maprotiline, ondansetron, propafenone, domperidone, quinacrine, ketoconazole, verapamil, tacrine, and salmeterol. tha 381-388 aldehyde oxidase 1 Homo sapiens 55-71 12939598-1 2003 After several weeks of treatment, levels of alanine aminotransferase (ALT) increase in 50% of patients treated with tacrine for Alzheimer"s disease. tha 116-123 glutamic--pyruvic transaminase Homo sapiens 44-68 12851386-6 2003 The advantages of this tethering were demonstrated with H287C AChE modified with six compounds, consisting of cationic trialkylammonium, acridinium, and tacrine ligands with tethers of varying length. tha 153-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 62-66 12939598-8 2003 After 12 to 28 days of treatment, administration of tacrine increased p53, Bax, mitochondrial permeability transition, cytosolic cytochrome c, and caspase-3 activity and triggered hepatocyte apoptosis and/or necrosis. tha 52-59 transformation related protein 53, pseudogene Mus musculus 70-73 12939598-8 2003 After 12 to 28 days of treatment, administration of tacrine increased p53, Bax, mitochondrial permeability transition, cytosolic cytochrome c, and caspase-3 activity and triggered hepatocyte apoptosis and/or necrosis. tha 52-59 BCL2-associated X protein Mus musculus 75-78 12939598-8 2003 After 12 to 28 days of treatment, administration of tacrine increased p53, Bax, mitochondrial permeability transition, cytosolic cytochrome c, and caspase-3 activity and triggered hepatocyte apoptosis and/or necrosis. tha 52-59 caspase 3 Mus musculus 147-156 12871155-4 2003 The BuChE inhibitory activity is only significant in compounds 11 and 14, ten-fold less active than tacrine. tha 100-107 butyrylcholinesterase Homo sapiens 4-9 12898628-2 2003 BChE was efficiently inhibited in a time- and concentration-dependent manner, and the enzyme could be protected against inhibition by active-site-specific ligands (that is, tacrine). tha 173-180 butyrylcholinesterase Homo sapiens 0-4 12914543-1 2003 The current pharmacological treatment of Alzheimer"s disease (AD) comes down to four marketed drugs (tacrine, donepezil, rivastigmine and galantamine) all of which are cholinesterase inhibitors, conforming to the cholinergic hypothesis. tha 101-108 butyrylcholinesterase Homo sapiens 168-182 12860300-6 2003 The results suggest that oral administration of PPE and tacrine increases acetylcholine concentration in the synaptic cleft of the hippocampus mostly through AChE inhibition, and that PPE has a potent and long-lasting effect on the central cholinergic system. tha 56-63 acetylcholinesterase Rattus norvegicus 158-162 12734391-5 2003 Among AChE inhibitors examined, donepezil and certain AChE inhibitors such as tacrine and galanthamine showed potent neuroprotective action, although physostigmine did not affect glutamate neurotoxicity. tha 78-85 acetylcholinesterase Rattus norvegicus 6-10 12734391-5 2003 Among AChE inhibitors examined, donepezil and certain AChE inhibitors such as tacrine and galanthamine showed potent neuroprotective action, although physostigmine did not affect glutamate neurotoxicity. tha 78-85 acetylcholinesterase Rattus norvegicus 54-58 12845416-3 2003 We investigated the effects on cognitive performance of combined treatments of ondansetron with either flumazenil, a GABA(A) receptor benzodiazepine site antagonist, or tacrine, a cholinesterase inhibitor, which are also able to prevent scopolamine-induced cognitive impairment. tha 169-176 butyrylcholinesterase Rattus norvegicus 180-194 12566177-0 2003 Cerebral glucose metabolism, cerebrospinal fluid-beta-amyloid1-42 (CSF-Abeta42), tau and apolipoprotein E genotype in long-term rivastigmine and tacrine treated Alzheimer disease (AD) patients. tha 145-152 apolipoprotein E Homo sapiens 89-105 12681373-3 2003 The two huprines were more active than both tacrine and (-)-huperzine A as inhibitors of both human and bovine AChE, and they acted as mixed-type AChE inhibitors. tha 44-51 acetylcholinesterase Bos taurus 111-115 12794390-2 2003 The kinetic effects of the cholinesterase inhibitors donepezil, galantamine, metrifonate, physostigmine, rivastigmine, and tetrahydroaminoacridine were examined with respect to their action on the esterase and aryl acylamidase activities of human acetylcholinesterase (AChE) and human butyrylcholinesterase (BuChE). tha 123-146 butyrylcholinesterase Homo sapiens 27-41 12725856-1 2003 The first X-ray structure of human carboxylesterase 1 (hCE1) and the structures of hCE1 with drug analogs bound reveal important molecular details of how the drugs cocaine, heroin, and tacrine are metabolized and cleared. tha 185-192 carboxylesterase 1 Homo sapiens 35-53 12725856-1 2003 The first X-ray structure of human carboxylesterase 1 (hCE1) and the structures of hCE1 with drug analogs bound reveal important molecular details of how the drugs cocaine, heroin, and tacrine are metabolized and cleared. tha 185-192 carboxylesterase 1 Homo sapiens 55-59 12725856-1 2003 The first X-ray structure of human carboxylesterase 1 (hCE1) and the structures of hCE1 with drug analogs bound reveal important molecular details of how the drugs cocaine, heroin, and tacrine are metabolized and cleared. tha 185-192 carboxylesterase 1 Homo sapiens 83-87 12725862-0 2003 Crystal structure of human carboxylesterase 1 complexed with the Alzheimer"s drug tacrine: from binding promiscuity to selective inhibition. tha 82-89 carboxylesterase 1 Homo sapiens 27-45 12725862-2 2003 We determined the 2.4 A crystal structure of hCE1 in complex with tacrine, the first drug approved for treating Alzheimer"s disease, and compare this structure to the Torpedo californica acetylcholinesterase (AcChE)-tacrine complex. tha 66-73 carboxylesterase 1 Homo sapiens 45-49 12725862-2 2003 We determined the 2.4 A crystal structure of hCE1 in complex with tacrine, the first drug approved for treating Alzheimer"s disease, and compare this structure to the Torpedo californica acetylcholinesterase (AcChE)-tacrine complex. tha 216-223 carboxylesterase 1 Homo sapiens 45-49 12725862-3 2003 Tacrine binds in multiple orientations within the catalytic gorge of hCE1, while it stacks in the smaller AcChE active site between aromatic side chains. tha 0-7 carboxylesterase 1 Homo sapiens 69-73 12725862-5 2003 Further, we use our structure to identify tacrine derivatives that act as low-micromolar inhibitors of hCE1 and may provide new avenues for treating narcotic abuse and cholesterol-related diseases. tha 42-49 carboxylesterase 1 Homo sapiens 103-107 12502352-2 2003 Tacrine-based AChE and BuChE inhibitors were designed by investigating the topology of the active site gorge of the two enzymes. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-18 12589378-10 2003 the AChE inhibitors tacrine and donepezil differ in their ability to modify muscarinic-receptor-mediated function in vivo. tha 20-27 acetylcholinesterase Rattus norvegicus 4-8 14535624-6 2003 Among these inhibitors, tacrine, bis-tacrine, TAK-147, metrifonate and galantamine inhibited both the G1 and G4 AChE forms equally well. tha 24-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 112-116 14533945-5 2003 The four cholinesterase inhibitors (tacrine, donepezil, rivastigmine and galantamine) that are currently available have different pharmacological properties that expose patients to the risk of several types of drug interactions of nonequivalent clinical relevance. tha 36-43 butyrylcholinesterase Homo sapiens 9-23 14533945-6 2003 The principal proven clinically relevant drug interactions involve tacrine and drugs metabolised by the cytochrome P450 (CYP) 1A2 enzyme, as well as tacrine or donepezil and antipsychotics (which results in the appearance of parkinsonian symptoms). tha 67-74 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 104-129 12445575-2 2002 In general, huperzine A preferentially inhibited tetrameric acetylcholinesterase (G4 form), while tacrine and rivastigmine preferentially inhibited monomeric acetylcholinesterase (G1 form). tha 98-105 acetylcholinesterase Rattus norvegicus 158-178 12445575-6 2002 The potent inhibitors of cortical G1 acetylcholinesterase were donepezil (K(i) 3.5 x 10(-9) M) and tacrine (K(i) 2.3 x 10(-8) M). tha 99-106 acetylcholinesterase Rattus norvegicus 37-57 12445575-7 2002 In hippocampus, huperzine A and physostigmine were the most potent inhibitors of G4 acetylcholinesterase, while donepezil and tacrine were most potent against G1 acetylcholinesterase. tha 126-133 acetylcholinesterase Rattus norvegicus 162-182 12480791-4 2002 In the clinical trial of tacrine, a first developed cholinesterase inhibitor, three cases markedly improved and, several years later, they were pathologically confirmed as dementia with Lewy bodies (DLB). tha 25-32 butyrylcholinesterase Homo sapiens 52-66 12198092-6 2002 Concentration dependence of closed-times is not predicted by sequential models of channel block, suggesting that tacrine blocks the nAChR by an unusual mechanism. tha 113-120 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 132-137 12414117-1 2002 The present studies investigated the effects of tacrine, a selective acetylcholinesterase (AChE) inhibitor and promising anti-dementia agent, on hydrogen peroxide (H(2)O(2))-induced apoptosis and the expression of apoptosis-related genes in rat pheochromocytoma line PC12 cells. tha 48-55 acetylcholinesterase Rattus norvegicus 69-89 12414117-5 2002 Preincubation with tacrine significantly attenuated H(2)O(2)-induced injury, prevented the cells from apoptosis and attenuated H(2)O(2)-induced overexpression of bax and p53. tha 19-26 BCL2 associated X, apoptosis regulator Rattus norvegicus 162-165 12414117-5 2002 Preincubation with tacrine significantly attenuated H(2)O(2)-induced injury, prevented the cells from apoptosis and attenuated H(2)O(2)-induced overexpression of bax and p53. tha 19-26 Wistar clone pR53P1 p53 pseudogene Rattus norvegicus 170-173 12134101-8 2002 11betaHSD2 activity was assessed by determining the ratio of corticosterone to dehydrocorticosterone metabolites (THB+5alphaTHB)/THA in urine. tha 129-132 hydroxysteroid 11-beta dehydrogenase 2 Rattus norvegicus 0-10 12196650-11 2002 The persistent CSF inhibition contrasts with earlier findings after long-term treatment by the reversible ChE inhibitor tacrine, which demonstrated increased AChE activity in the CSF but not in the blood. tha 120-127 butyrylcholinesterase Homo sapiens 106-109 12196650-11 2002 The persistent CSF inhibition contrasts with earlier findings after long-term treatment by the reversible ChE inhibitor tacrine, which demonstrated increased AChE activity in the CSF but not in the blood. tha 120-127 acetylcholinesterase (Cartwright blood group) Homo sapiens 158-162 11863435-9 2002 Furthermore, both tacrine and huprine X bind more tightly to Torpedo than to human AChE, suggesting that their quinoline substructures interact better with Phe330 than with Tyr337, the corresponding residue in the human AChE structure. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 12083745-2 2002 The earliest known ChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of AD patients. tha 61-68 butyrylcholinesterase Homo sapiens 19-22 12207285-3 2002 These compounds are competitive inhibitors for acetylcholinesterase, the more potent being compound (13) which is three-fold less active than tacrine. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-67 12207285-4 2002 The butyrylcholinesterase inhibition activity is significant only in compounds 10 and133, which are ten-fold less active than tacrine. tha 126-133 butyrylcholinesterase Homo sapiens 4-25 12139368-4 2002 Tacrine and rivastigmine inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the CSF of Alzheimer"s disease patients. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-58 12139368-4 2002 Tacrine and rivastigmine inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in the CSF of Alzheimer"s disease patients. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-64 12134305-6 2002 Up to now, although with limited success, this improvement has been achieved only with the reversible inhibitors of acetylcholinesterase tacrine, rivastigmine and donepezil, available in the clinic since a few years. tha 137-144 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-136 12014965-2 2002 Heptylene-linked bis-(6-chloro)tacrine (3h) was found up to 3000- and 3-fold more potent in inhibiting rat AChE than tacrine and the unsubstituted bis-tacrine 3b, respectively. tha 31-38 acetylcholinesterase Rattus norvegicus 107-111 12014965-3 2002 Changes in the size of the carbocyclic ring of the dimeric tacrine reduced both the selectivity and the potency of AChE inhibition as compared to 3b. tha 59-66 acetylcholinesterase Rattus norvegicus 115-119 12014965-5 2002 The pronounced enhancement of AChE inhibition potency and AChE/BChE selectivity was achieved with incorporation of a halogen at the 6-position of homodimeric tacrines. tha 158-166 acetylcholinesterase Rattus norvegicus 30-34 12014965-5 2002 The pronounced enhancement of AChE inhibition potency and AChE/BChE selectivity was achieved with incorporation of a halogen at the 6-position of homodimeric tacrines. tha 158-166 acetylcholinesterase Rattus norvegicus 58-62 12014965-5 2002 The pronounced enhancement of AChE inhibition potency and AChE/BChE selectivity was achieved with incorporation of a halogen at the 6-position of homodimeric tacrines. tha 158-166 butyrylcholinesterase Rattus norvegicus 63-67 11863435-9 2002 Furthermore, both tacrine and huprine X bind more tightly to Torpedo than to human AChE, suggesting that their quinoline substructures interact better with Phe330 than with Tyr337, the corresponding residue in the human AChE structure. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 220-224 11846398-2 2002 Here we report Western blotting evidence demonstrating that in rat LiCl and tacrine enhance the expression of neuronal nitric oxide synthase (nNOS), but not eNOS, enzyme protein in the hippocampus during the preconvulsive period and this triggers seizures and hippocampal damage. tha 76-83 nitric oxide synthase 1 Rattus norvegicus 110-140 11846398-2 2002 Here we report Western blotting evidence demonstrating that in rat LiCl and tacrine enhance the expression of neuronal nitric oxide synthase (nNOS), but not eNOS, enzyme protein in the hippocampus during the preconvulsive period and this triggers seizures and hippocampal damage. tha 76-83 nitric oxide synthase 1 Rattus norvegicus 142-146 11928722-2 2002 T-82, tacrine and E2020 all concentration-dependently inhibited AChE in rat brain homogenate (IC50 = 109.4, 84.2 and 11.8 nM, respectively). tha 6-13 acetylcholinesterase Rattus norvegicus 64-68 11804611-5 2002 Further, fluoxetine, with and without WAY 100635, markedly potentiated the effectiveness of the acetylcholinesterase (AChE) inhibitor tacrine (5 mg/kg) to restore EEG activation between 4-30 Hz. tha 134-141 acetylcholinesterase Rattus norvegicus 96-116 11953120-15 2002 Tha mechanism may be down-regulation of MMP-2 expression and decrease of tumor angiogenesis. tha 0-3 matrix metallopeptidase 2 Homo sapiens 40-45 12362625-21 2002 Emphasis is put on the preoperative treatment by human recombinant erythropoietin and hematopoietics, a careful approach during THA with the reduction of the surgery duration and maintenance of normothermia intraoperatively. tha 128-131 erythropoietin Homo sapiens 67-81 12162759-3 2002 Tacrine was the first cholinesterase inhibitor approved by regulatory agencies, followed by donepezil, rivastigmine and recently galantamine. tha 0-7 butyrylcholinesterase Homo sapiens 22-36 12162759-7 2002 Tacrine is metabolised by hepatic cytochrome P450 (CYP) 1A2, and donepezil and galantamine are metabolised by CYP3A4 and CYP2D6. tha 0-7 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-59 12218259-3 2002 To test the hypothesis that treatment with a cholinesterase inhibitor could change the levels of Abeta in plasma, we measured Abeta42 and Abeta40 plasma levels in AD subjects before tacrine treatment and at weeks 2 and 6 of treatment. tha 182-189 butyrylcholinesterase Homo sapiens 45-59 11804611-5 2002 Further, fluoxetine, with and without WAY 100635, markedly potentiated the effectiveness of the acetylcholinesterase (AChE) inhibitor tacrine (5 mg/kg) to restore EEG activation between 4-30 Hz. tha 134-141 acetylcholinesterase Rattus norvegicus 118-122 11095509-1 2000 The acetylcholinesterase inhibitor tacrine and the monoamine oxidase inhibitor deprenyl are considered useful pharmacotherapies for Alzheimer"s disease (AD). tha 35-42 acetylcholinesterase Rattus norvegicus 4-24 11563919-1 2001 Chimeras of tacrine and m-(N,N,N-Trimethylammonio)trifluoroacetophenone (1) were designed as novel, reversible inhibitors of acetylcholinesterase. tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-145 11495583-5 2001 Moreover, 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-5-methyl-6-phenylpyridazine 4c, which showed an IC(50) of 21 nM, is 100-times more selective for human AChE (human BuChE/AChE ratio of 24) than the reference compound tacrine. tha 218-225 acetylcholinesterase (Cartwright blood group) Homo sapiens 154-158 11495583-5 2001 Moreover, 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-5-methyl-6-phenylpyridazine 4c, which showed an IC(50) of 21 nM, is 100-times more selective for human AChE (human BuChE/AChE ratio of 24) than the reference compound tacrine. tha 218-225 acetylcholinesterase (Cartwright blood group) Homo sapiens 172-176 12369981-0 2001 Tacrine-huperzine A hybrids (huprines): a new class of highly potent and selective acetylcholinesterase inhibitors of interest for the treatment of Alzheimer"s disease. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-103 12369981-1 2001 Tacrine-huperzine A hybrids (huprines) are a new class of very potent and selective acetylcholinesterase (AChE) inhibitors. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-104 12369981-1 2001 Tacrine-huperzine A hybrids (huprines) are a new class of very potent and selective acetylcholinesterase (AChE) inhibitors. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-110 12585078-3 2001 RESULTS: The alteration of mice body temperature, and the elevation of serum ALT, liver MDA content, and mitochondria potential induced by THA were significantly inhibited by DDB pretreatment. tha 139-142 glutamic pyruvic transaminase, soluble Mus musculus 77-80 12585078-5 2001 On the other hand, The inhibiting effects of THA on mice hippocampus and cortex acetylcholinesterase in vitro and in vivo were not influenced by DDB treatment. tha 45-48 acetylcholinesterase Mus musculus 80-100 11508052-0 2001 [Detection of the cholinesterase inhibitor tacrine and its main metabolites]. tha 43-50 butyrylcholinesterase Homo sapiens 18-32 11508052-1 2001 Tacrine, a cholinesterase inhibitor for symptomatic treatment of minor to moderate dementia, and its primary metabolites 1-hydroxy-tacrine and 4-hydroxy-tacrine were studied by means of thin-layer chromatography, UV spectroscopy and gas-chromatography/mass spectroscopy. tha 0-7 butyrylcholinesterase Homo sapiens 11-25 11330337-8 2001 Moreover, the rank order for potency in inhibiting acetylcholinesterase (ambenonium>neostigmine=physostigmine =tacrine>pyridostigmine=edrophonium=galanthamine >desoxypeganine>parathion>gramine) indicated that the most effective inhibitors of acetylcholinesterase also displaced [3H]-oxotremorine-M to the greatest extent. tha 114-121 acetylcholinesterase Rattus norvegicus 51-71 11979067-2 2002 Thirteen patients, 6 currently receiving treatment with the cholinesterase inhibitor tacrine (tetrahydroaminoacridine; THA) and the remaining being medication free, were administered 2 mg of nicotine polacrilex under double-blind, randomized, placebo-controlled conditions. tha 85-92 butyrylcholinesterase Homo sapiens 60-74 11684153-1 2001 Tacrine, a reversible cholinesterase (ChE) inhibitor, lowers body temperature by increasing cholinergic activity in the hypothalamus. tha 0-7 butyrylcholinesterase Rattus norvegicus 22-36 11684153-1 2001 Tacrine, a reversible cholinesterase (ChE) inhibitor, lowers body temperature by increasing cholinergic activity in the hypothalamus. tha 0-7 butyrylcholinesterase Rattus norvegicus 38-41 11684153-7 2001 Plasma ChE can bind tacrine thereby lowering the amount available to the brain. tha 20-27 butyrylcholinesterase Rattus norvegicus 7-10 11679020-2 2001 The reversible cholinesterase inhibitor, tacrine (THA) was examined against the contractions of rat duodenum to acetylcholine and carbachol (cholinesterase resistant). tha 41-48 butyrylcholinesterase Rattus norvegicus 15-29 11679020-2 2001 The reversible cholinesterase inhibitor, tacrine (THA) was examined against the contractions of rat duodenum to acetylcholine and carbachol (cholinesterase resistant). tha 41-48 butyrylcholinesterase Rattus norvegicus 141-155 11679020-10 2001 Further evidence for muscarininc receptor antagonism by tacrine was a small rightward shift of the concentration-response curve for carbachol, an agonist immune to cholinesterase. tha 56-63 butyrylcholinesterase Rattus norvegicus 164-178 11679020-12 2001 This study has shown that tacrine acts both as a cholinesterase inhibitor and muscarinic antagonist on rat intestinal smooth muscle. tha 26-33 butyrylcholinesterase Rattus norvegicus 49-63 11310608-0 2001 Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of new tacrine-like analogues. tha 84-91 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-34 11310608-0 2001 Synthesis and acetylcholinesterase/butyrylcholinesterase inhibition activity of new tacrine-like analogues. tha 84-91 butyrylcholinesterase Homo sapiens 35-56 11230879-6 2001 We have found that a subgroup of cholinesterase inhibitors, including galantamine but excluding tacrine, directly interacts with nicotinic acetylcholine receptors. tha 96-103 butyrylcholinesterase Homo sapiens 33-47 11893059-2 2001 The earliest known AChE inhibitors, namely, physostigmine and tacrine, performed poorly in clinical trials (e.g., poor oral activity, brain penetration, and hepatotoxic liability). tha 62-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-23 11125238-0 2001 Responder characteristics to a single oral dose of cholinesterase inhibitor: a double-blind placebo-controlled study with tacrine in Alzheimer patients. tha 122-129 butyrylcholinesterase Homo sapiens 51-65 11475012-0 2001 Tacrine and rate of progression in Alzheimer"s disease--relation to ApoE allele genotype. tha 0-7 apolipoprotein E Homo sapiens 68-72 11475012-6 2001 The results primarily suggest a faster rate of decline in the ApoE4 AD compared to the ApoE2-3, but may also reflect that ApoE epsilon4 genotype inheritance is a negative predictor of treatment effect of tacrine in AD patients. tha 204-211 apolipoprotein E Homo sapiens 62-66 11150921-28 2001 Moreover, the increase in plasma adrenaline and vasopressin levels appears to be involved in the pressor effect of THA. tha 115-118 arginine vasopressin Rattus norvegicus 48-59 11101357-0 2000 New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer"s disease. tha 4-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 11101357-1 2000 Several new 12-amino-6,7,10,11-tetrahydro-7, 11-methanocycloocta[b]quinoline derivatives (tacrine-huperzine A hybrids, huprines) have been synthesized and tested as acetylcholinesterase (AChE) inhibitors. tha 90-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 165-185 11101357-1 2000 Several new 12-amino-6,7,10,11-tetrahydro-7, 11-methanocycloocta[b]quinoline derivatives (tacrine-huperzine A hybrids, huprines) have been synthesized and tested as acetylcholinesterase (AChE) inhibitors. tha 90-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 187-191 11121617-2 2000 The acetylcholinesterase (AChE) inhibitory activity of all compounds was measured using Ellman"s method and some of them turned out to be as potent as tacrine. tha 151-158 acetylcholinesterase Rattus norvegicus 4-24 11121617-2 2000 The acetylcholinesterase (AChE) inhibitory activity of all compounds was measured using Ellman"s method and some of them turned out to be as potent as tacrine. tha 151-158 acetylcholinesterase Rattus norvegicus 26-30 10943943-3 2000 Tacrine significantly increased the value of deltaG, deltaH, deltaH*, Q10, Ea and PZ factor, and decreased the value of deltaS for AChE. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-135 11256231-4 2000 The order of inhibitory potency (IC50) towards AChE activity under optimal assay conditions for each ChE inhibitor was: physostigmine (0.67 nM) > rivastigmine (4.3 nM) > donepezil (6.7 nM) > TAK-147 (12 nM) > tacrine (77 nM) > ipidacrine (270 nM). tha 209-216 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-51 11256231-4 2000 The order of inhibitory potency (IC50) towards AChE activity under optimal assay conditions for each ChE inhibitor was: physostigmine (0.67 nM) > rivastigmine (4.3 nM) > donepezil (6.7 nM) > TAK-147 (12 nM) > tacrine (77 nM) > ipidacrine (270 nM). tha 209-216 butyrylcholinesterase Homo sapiens 48-51 10915830-3 2000 Amitriptyline, carbamazepine, chlorpromazine, cyproheptadine, imipramine, tacrine and trifluperazine blocked SK2 channel currents with micromolar affinity. tha 74-81 potassium calcium-activated channel subfamily N member 2 Rattus norvegicus 109-112 11098729-8 2000 The ADAS-Cog has become the standard instrument since it was used for the approval of tacrine and other cholinesterase inhibitors. tha 86-93 alkylglycerone phosphate synthase Homo sapiens 4-8 10996445-5 2000 The above-mentioned neuroprotective effects are also observed with tacrine (1 microM), donepezil (10 microM) and galanthamine (10 microM), suggesting that the neuroprotective effects of cholinesterase inhibitor might partly contribute to the clinical efficacy in AD treatment. tha 67-74 butyrylcholinesterase Rattus norvegicus 186-200 11029868-3 2000 The cholinesterase inhibitors (tacrine, donepezil, and rivastigmine) are the only FDA-approved class of medications for AD. tha 31-38 butyrylcholinesterase Homo sapiens 4-18 10956426-5 2000 Pretreatment of the cells with HupA or tacrine (0.1-10 microM) prior to Abeta exposure significantly elevated the cell survival and GSH-Px and CAT activities and decreased the level of MDA. tha 39-46 catalase Rattus norvegicus 143-146 11343620-3 2000 Nevertheless, symptomatic relief is a feasible treatment option for AD patients and is available currently in the form of cholinesterase inhibitors such as tacrine, donepezil, metrifonate and rivastigmine. tha 156-163 butyrylcholinesterase Homo sapiens 122-136 10943943-4 2000 Since there is no known report on the inhibition of human retinal AChE by tacrine, these results were compared with the reported values for the energy parameters of camel retinal and chicken brain AChE inhibition by an anti-cancer drug, cyclophosphamide. tha 74-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 10837930-1 2000 For the first time, kinetic parameters of the effect of tacrine, an anti-cholinesterase inhibitor of therapeutic potential in Alzheimer"s disease has been studied on human retinal acetyl-cholinesterase (AChE). tha 56-63 butyrylcholinesterase Homo sapiens 73-87 22033801-3 2000 Five such agents are reviewed: tacrine and donepezil, which act at the ionic subsite of acetylcholinesterase (AChE), and rivastigmine, galantamine, and metrifonate, which act at its catalytic esteratic subsite. tha 31-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-108 22033801-3 2000 Five such agents are reviewed: tacrine and donepezil, which act at the ionic subsite of acetylcholinesterase (AChE), and rivastigmine, galantamine, and metrifonate, which act at its catalytic esteratic subsite. tha 31-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-114 22034442-6 2000 Cholinesterase inhibitors, including donepezil, tacrine, rivastigmine, and galantamine are the recommended treatment of cognitive disturbance in patients with Alzheimer"s disease. tha 48-55 butyrylcholinesterase Homo sapiens 0-14 10821713-0 2000 SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. tha 7-41 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 10821713-0 2000 SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. tha 155-162 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 10821713-1 2000 In this study, we attempted to derive a comprehensive SAR picture for the class of acetylcholinesterase (AChE) inhibitors related to tacrine, a drug currently in use for the treatment of the Alzheimer"s disease. tha 133-140 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-103 10821713-1 2000 In this study, we attempted to derive a comprehensive SAR picture for the class of acetylcholinesterase (AChE) inhibitors related to tacrine, a drug currently in use for the treatment of the Alzheimer"s disease. tha 133-140 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 10821713-4 2000 The three-dimensional (3D) properties of the inhibitors were taken into consideration by performing a CoMFA analysis on the series of AChE inhibitors made by 12 9-amino-1,2,3, 4-tetrahydroacridines and 13 11H-indeno[1,2-b]quinolin-10-ylamines previously developed in our laboratory. tha 161-197 acetylcholinesterase (Cartwright blood group) Homo sapiens 134-138 10837930-1 2000 For the first time, kinetic parameters of the effect of tacrine, an anti-cholinesterase inhibitor of therapeutic potential in Alzheimer"s disease has been studied on human retinal acetyl-cholinesterase (AChE). tha 56-63 butyrylcholinesterase Homo sapiens 187-201 10762042-2 2000 Compounds 6b-c were found to be more potent than galanthamine and tacrine in inhibiting AChE. tha 66-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-92 10817586-0 2000 Tacrine, a reversible acetylcholinesterase inhibitor, induces myopathy. tha 0-7 acetylcholinesterase Rattus norvegicus 22-42 10817586-1 2000 Tacrine, an acetylcholinesterase (AChE) inhibitor that has been used in the treatment of Alzheimer"s disease, increases available acetylcholine (Ach) levels in the synaptic cleft thereby enhancing the activity of cholinergic pathways. tha 0-7 acetylcholinesterase Rattus norvegicus 12-32 10817586-1 2000 Tacrine, an acetylcholinesterase (AChE) inhibitor that has been used in the treatment of Alzheimer"s disease, increases available acetylcholine (Ach) levels in the synaptic cleft thereby enhancing the activity of cholinergic pathways. tha 0-7 acetylcholinesterase Rattus norvegicus 34-38 10817586-3 2000 We tested whether reversible AChE inhibitors such as tacrine may induce similar effects. tha 53-60 acetylcholinesterase Rattus norvegicus 29-33 10886308-0 2000 The apolipoprotein E epsilon4 allele and the response to tacrine therapy in Alzheimer"s disease. tha 57-64 apolipoprotein E Homo sapiens 4-20 10886308-1 2000 The objective of our study was to evaluate the effects of the apolipoprotein E (ApoE) phenotype and gender on the response to tacrine treatment in Alzheimer"s disease (AD). tha 126-133 apolipoprotein E Homo sapiens 62-78 10886308-1 2000 The objective of our study was to evaluate the effects of the apolipoprotein E (ApoE) phenotype and gender on the response to tacrine treatment in Alzheimer"s disease (AD). tha 126-133 apolipoprotein E Homo sapiens 80-84 10886308-2 2000 ApoE phenotyping was performed on 76 patients treated with tacrine for AD. tha 59-66 apolipoprotein E Homo sapiens 0-4 10637365-3 2000 These data are summarised from nearly all therapeutically important chemical classes of reversible AChE inhibitors, e.g., derivatives of physostigmine, tacrine, donepezil and huperzine A. Interactions observed from X-ray crystallography between these inhibitors and AChE have also been incorporated and compared with modelling and QSAR results. tha 152-159 acetylcholinesterase (Cartwright blood group) Homo sapiens 99-103 10801254-1 2000 BACKGROUND: Glutathione conjugation of tacrine reactive metabolites depends in part on the activity of glutathione-S-transferases (GST), of which two isozymes (GST M1 and GST T1) are polymorphically expressed. tha 39-46 glutathione S-transferase theta 1 Homo sapiens 171-177 10717417-1 2000 The novel dimer bis(7)-tacrine (1,7-N-Heptylene-bis-9,9"-amino-1,2,3, 4-tetrahydroacridine), which exhibits higher potency, selectivity and oral activity on acetylcholinesterase inhibition in vivo than tacrine, was evaluated for its ability to reverse AF64A-induced spatial memory impairment in rats using the Morris water maze. tha 23-30 acetylcholinesterase Rattus norvegicus 157-177 10637367-3 2000 The earliest known AChE inhibitors, namely, physostigmine and tacrine, showed modest improvement in the cognitive function of Alzheimer"s patients. tha 62-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-23 11273593-5 2000 Current approved AD drugs, such as aricept and tacrine, are based on the use of cholinesterase inhibitors (ChEIs) and have been reported to improve memory deficits and cognitive decline in some patients with AD. tha 47-54 butyrylcholinesterase Homo sapiens 80-94 10849895-1 2000 Previous investigations have indicated that a single dose pharmaco-EEG may predict the outcome of 4-7 weeks of tetrahydroaminoacridine (THA) treatment in dementia of the Alzheimer type (DAT). tha 111-134 solute carrier family 6 member 3 Homo sapiens 186-189 10849895-1 2000 Previous investigations have indicated that a single dose pharmaco-EEG may predict the outcome of 4-7 weeks of tetrahydroaminoacridine (THA) treatment in dementia of the Alzheimer type (DAT). tha 136-139 solute carrier family 6 member 3 Homo sapiens 186-189 10688981-4 2000 Oral administration of donepezil, tacrine, ENA-713 or TAK-147, caused a dose-dependent inhibition of brain and plasma cholinesterase activities. tha 34-41 butyrylcholinesterase Rattus norvegicus 118-132 10646530-3 2000 Western blot analysis showed that treatment of SH-SY5Y cells for 72 h with the cholinesterase inhibitors tacrine (10(-5) M), donepezil (10(-5) M), and galanthamine (10(-5) M), nicotine (10(-5) M), and epibatidine (10(-7) M) increased tau levels as detected with Tau-1, AT 8, and AT 270 monoclonal antibodies and binding of [3H]epibatidine. tha 105-112 butyrylcholinesterase Homo sapiens 79-93 10648652-2 2000 Huperzine A, a natural product used in traditional Chinese herbal medicine, and tacrine (Cognex) are among the potent AChE inhibitors used in this treatment, but the search for more selective inhibitors continues. tha 80-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-122 10648652-2 2000 Huperzine A, a natural product used in traditional Chinese herbal medicine, and tacrine (Cognex) are among the potent AChE inhibitors used in this treatment, but the search for more selective inhibitors continues. tha 89-95 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-122 11034705-3 2000 Tacrine, the first of the cholinesterase inhibitors to undergo extensive trials for this purpose, was associated with significant adverse effects including hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 26-40 16787838-8 2000 Pretreatment of PC12 cells with cholinesterase inhibitors such as tacrine and donepezil in clinical relevant concentrations can attenuate Abeta (25-35) toxicity through mechanisms which may be mediated via nicotinic receptors. tha 66-73 butyrylcholinesterase Rattus norvegicus 32-46 10641971-2 2000 Tacrine and donepezil are classified as short-acting or reversible agents since binding to acetylcholinesterase enzyme (AChE) is hydrolyzed within minutes. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 91-118 10641971-2 2000 Tacrine and donepezil are classified as short-acting or reversible agents since binding to acetylcholinesterase enzyme (AChE) is hydrolyzed within minutes. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 120-124 10602696-1 1999 The binding of the 9-methyl derivative of tacrine-huperzine A hybrid to Torpedo californica acetylcholinesterase (AChE) has been studied by computational methods. tha 42-49 acetylcholinesterase (Cartwright blood group) Homo sapiens 114-118 10794858-3 2000 The acetylcholinesterase inhibitor tacrine, at doses between 10 and 20 mg/kg, reversed these EEG changes; co-administration of tacrine and the noradrenaline-serotonin reuptake inhibitor imipramine (10 mg/kg) enhanced tacrine"s action to suppress delta activity. tha 35-42 acetylcholinesterase Rattus norvegicus 4-24 10602696-8 1999 Overall, the whole of results supports the validity of the putative binding model to explain the binding of tacrine-huperzine A hybrids to AChE. tha 108-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 10611458-7 1999 Tacrine, at doses of 5, 10 and 20 mg/kg, p.o., dose-dependently inhibited cholinesterase activity in all tissues of both young and aged animals, but most potently in heart, small intestine and liver. tha 0-7 butyrylcholinesterase Rattus norvegicus 74-88 10611458-8 1999 The inhibition of cholinesterase activity by tacrine in the brain, plasma, erythrocytes, heart and liver was more potent in aged rats than in tissues of young rats. tha 45-52 butyrylcholinesterase Rattus norvegicus 18-32 10611458-2 1999 In the present study, its inhibitory effect on the activity of cholinesterase ex vivo was evaluated in the brain, plasma, erythrocytes, heart, small intestine, liver and pectoral muscle of young adult as well as aged rats, in comparison with that of tacrine (9-amino-1,2,3,4-tetrahydroacridine hydrochloride). tha 250-257 butyrylcholinesterase Rattus norvegicus 63-77 10611458-11 1999 It is concluded that the inhibitory effects of donepezil and tacrine on cholinesterase activity are greater in aged than in young rats, owing to differences in the tissue concentrations of these compounds between young and aged animals. tha 61-68 butyrylcholinesterase Rattus norvegicus 72-86 10622674-8 1999 A number of preliminary studies, whose results are summarized here, have demonstrated that the use of the acetylcholinesterase inhibitors tacrine, metrifonate and donepezil, and the glial cell modulator, propentofylline, results in reductions in the overall costs of care. tha 138-145 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 10613616-12 1999 This interaction between tacrine and HRT involves reduced metabolic conversion of tacrine to its main metabolite 1-hydroxytacrine by CYP1A2 during the first-pass phase. tha 25-32 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 133-139 10613616-12 1999 This interaction between tacrine and HRT involves reduced metabolic conversion of tacrine to its main metabolite 1-hydroxytacrine by CYP1A2 during the first-pass phase. tha 82-89 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 133-139 10594314-3 1999 Tacrine (12.5 and 17.7 mg/kg) produced significantly less inhibition of cholinesterase in the hippocampus but more in the striatum than rivastigmine (0.75 and 1.5 mg/kg) and only antagonised the deficit in reference memory. tha 0-7 butyrylcholinesterase Rattus norvegicus 72-86 10619655-4 1999 The action of AChE was not affected by edrophonium and tacrine both active site inhibitors, but it was abolished by propidium and gallamine, two peripheral anionic binding site (PAS) ligands. tha 55-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-18 11249555-4 1999 It is structurally dissimilar from other established cholinesterase inhibitors, namely THA (an acridine compound) and the carbamates, physostigmine and rivastigmine and has a pharmacokinetic and tolerability profile distinct from these agents. tha 87-90 butyrylcholinesterase Homo sapiens 53-67 10594467-1 1999 AIMS: The aim of the present study was to examine the CYP1A2 substrate tacrine as a possible alternative to caffeine for assessing CYP1A2 activity in vivo. tha 71-78 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 54-60 10594467-1 1999 AIMS: The aim of the present study was to examine the CYP1A2 substrate tacrine as a possible alternative to caffeine for assessing CYP1A2 activity in vivo. tha 71-78 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 131-137 10219924-5 1999 The cholinesterase inhibitors, tacrine and donepezil, are effective in improving cognition, delaying nursing home placement, and improving behavioral complications in some patients. tha 31-38 butyrylcholinesterase Homo sapiens 4-18 11139819-4 1999 Early acetylcholinesterase inhibitors, such as tacrine and physostigmine, are poorly tolerated and have a short duration of action. tha 47-54 acetylcholinesterase (Cartwright blood group) Homo sapiens 6-26 10534086-9 1999 Two cholinesterase inhibitors, tacrine and donepezil, are effective in treating cognitive and global function. tha 31-38 butyrylcholinesterase Homo sapiens 4-18 10514292-1 1999 Dimeric acetylcholinesterase (AChE) inhibitors containing a single 9-amino-1,2,3,4-tetrahydroacridine (tacrine) unit were constructed in an effort to further delineate structural requirements for optimal binding to the AChE peripheral site. tha 67-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 8-28 10514292-1 1999 Dimeric acetylcholinesterase (AChE) inhibitors containing a single 9-amino-1,2,3,4-tetrahydroacridine (tacrine) unit were constructed in an effort to further delineate structural requirements for optimal binding to the AChE peripheral site. tha 67-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 10514292-1 1999 Dimeric acetylcholinesterase (AChE) inhibitors containing a single 9-amino-1,2,3,4-tetrahydroacridine (tacrine) unit were constructed in an effort to further delineate structural requirements for optimal binding to the AChE peripheral site. tha 103-110 acetylcholinesterase (Cartwright blood group) Homo sapiens 8-28 10514292-1 1999 Dimeric acetylcholinesterase (AChE) inhibitors containing a single 9-amino-1,2,3,4-tetrahydroacridine (tacrine) unit were constructed in an effort to further delineate structural requirements for optimal binding to the AChE peripheral site. tha 103-110 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 10514292-3 1999 AChE IC(50) values of the optimum dimers decrease significantly as the peripheral site ligand was permuted in the series ammonia > dimethylamine > 4-aminopyridine > 4-aminoquinoline > tacrine. tha 196-203 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 10513568-9 1999 These results suggest that oral administration of donepezil, tacrine and ENA-713 increases acetylcholine concentration in the synaptic cleft of the hippocampus mostly through AChE inhibition, and that donepezil has a more potent activity than tacrine and a longer-lasting effect than ENA-713 on the central cholinergic system. tha 61-68 acetylcholinesterase Rattus norvegicus 175-179 10456487-1 1999 OBJECTIVE: In vitro studies have shown that tacrine is metabolized by cytochrome P4501A2 (CYP1A2). tha 44-51 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 70-88 10456487-1 1999 OBJECTIVE: In vitro studies have shown that tacrine is metabolized by cytochrome P4501A2 (CYP1A2). tha 44-51 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 90-96 10456487-3 1999 The aim of this study was to establish whether the potent CYP1A2 inhibitor fluvoxamine in clinically relevant doses could inhibit tacrine metabolism. tha 130-137 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 58-64 10332935-5 1999 Although ChE inhibitors appear to be the most promising, tacrine, the first ChE inhibitor to be registered and approved for the treatment of AD, has significant tolerability problems. tha 57-64 butyrylcholinesterase Homo sapiens 76-79 10096702-3 1999 To date, two reversible cholinesterase inhibitors-tacrine and donepezil-have been marketed. tha 50-57 butyrylcholinesterase Homo sapiens 24-38 10208549-2 1999 Based on IC50 ratios, the dimeric analog bis(7)-tacrine was, in a reversible manner, up to 150-fold more potent and 250-fold more selective than tacrine for acetylcholinesterase (AChE) over butyrylcholinesterase (BChE). tha 48-55 acetylcholinesterase Rattus norvegicus 157-177 10208549-2 1999 Based on IC50 ratios, the dimeric analog bis(7)-tacrine was, in a reversible manner, up to 150-fold more potent and 250-fold more selective than tacrine for acetylcholinesterase (AChE) over butyrylcholinesterase (BChE). tha 48-55 acetylcholinesterase Rattus norvegicus 179-183 10208549-2 1999 Based on IC50 ratios, the dimeric analog bis(7)-tacrine was, in a reversible manner, up to 150-fold more potent and 250-fold more selective than tacrine for acetylcholinesterase (AChE) over butyrylcholinesterase (BChE). tha 48-55 butyrylcholinesterase Rattus norvegicus 190-211 10208549-2 1999 Based on IC50 ratios, the dimeric analog bis(7)-tacrine was, in a reversible manner, up to 150-fold more potent and 250-fold more selective than tacrine for acetylcholinesterase (AChE) over butyrylcholinesterase (BChE). tha 48-55 butyrylcholinesterase Rattus norvegicus 213-217 10208549-3 1999 Following a single oral administration, both bis(7)-tacrine and tacrine produced dose-dependent inhibitions of AChE in rat brain, but bis(7)-tacrine exhibited higher efficacy and AChE/BChE selectivity than tacrine. tha 52-59 acetylcholinesterase Rattus norvegicus 111-115 10208549-3 1999 Following a single oral administration, both bis(7)-tacrine and tacrine produced dose-dependent inhibitions of AChE in rat brain, but bis(7)-tacrine exhibited higher efficacy and AChE/BChE selectivity than tacrine. tha 64-71 acetylcholinesterase Rattus norvegicus 111-115 10208549-3 1999 Following a single oral administration, both bis(7)-tacrine and tacrine produced dose-dependent inhibitions of AChE in rat brain, but bis(7)-tacrine exhibited higher efficacy and AChE/BChE selectivity than tacrine. tha 64-71 butyrylcholinesterase Rattus norvegicus 184-188 10208550-1 1999 Heptylene-linked bis-(9-amino-1,2,3,4-tetrahydroacridine) (bis(7)-tacrine) is a potential palliative therapeutic agent for Alzheimer"s disease (AD), on the basis of its superior acetylcholinesterase (AChE) inhibition and memory-enhancing potency relative to tacrine. tha 66-73 acetylcholinesterase Rattus norvegicus 200-204 10218828-5 1999 Finally, these studies indicate that simultaneous binding of alkylene-linked 9-amino-1,2,3,4-tetrahydroacridine dimers to the catalytic and peripheral sites of AChE is possible with a tether length as short as 5 methylenes. tha 77-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 10437161-6 1999 Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. tha 0-7 butyrylcholinesterase Mus musculus 54-59 10205783-7 1999 THA (9-amino-1,2,3,4-tetrahydroacridine), a cholinesterase inhibitor and GTS-21 (3-(2,4-dimethoxybenzylidene)-anabaseine dihydrochloride), a central nicotinic acetylcholine-receptor agonist improved the learning impairment in the radical maze task of 2VO rats. tha 0-3 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 149-181 9862746-9 1999 Because we documented that GAPDH overexpression participates in neuronal apoptosis induced by various insults, we conclude that the neuroprotective actions of ONO-1603 and THA appear to be mediated by suppression of this protein overexpression. tha 172-175 glyceraldehyde-3-phosphate dehydrogenase Rattus norvegicus 27-32 9989475-2 1999 Tetrahydroaminoacridine (tacrine, Cognex), a simple acridine, is a reversible inhibitor of cholinesterase activity available for the symptomatic treatment of Alzheimer"s disease. tha 0-23 butyrylcholinesterase Homo sapiens 91-105 9989475-2 1999 Tetrahydroaminoacridine (tacrine, Cognex), a simple acridine, is a reversible inhibitor of cholinesterase activity available for the symptomatic treatment of Alzheimer"s disease. tha 25-32 butyrylcholinesterase Homo sapiens 91-105 9989475-2 1999 Tetrahydroaminoacridine (tacrine, Cognex), a simple acridine, is a reversible inhibitor of cholinesterase activity available for the symptomatic treatment of Alzheimer"s disease. tha 34-40 butyrylcholinesterase Homo sapiens 91-105 9880090-5 1998 Three cholinesterase inhibitors, tacrine, donepezil and rivastigmine, are in clinical use. tha 33-40 butyrylcholinesterase Homo sapiens 6-20 10637939-9 1999 Cholinergic drugs including cholinesterase inhibitors such as physostigmine, tacrine, velnacrine as well as the acetylcholine releaser linopiridine have been reported to increase the cerebral blood flow in AD patients both after acute and fairly short period of treatment. tha 77-84 butyrylcholinesterase Homo sapiens 28-42 9813282-6 1998 In this study, we extended our studies by analysis of Abeta40 and Abeta42 and report that in a human neuroblastoma cell line tacrine reduced the levels of total Abeta, Abeta40 and Abeta42 in addition to sAPP. tha 125-132 amyloid beta precursor protein Homo sapiens 54-59 9868741-1 1998 The selective serotonin re-uptake inhibitor, fluvoxamine, is a very potent inhibitor of CYP1A2, and accordingly causes pharmacokinetic interactions with drugs metabolised by CYP1A2, such as caffeine, theophylline, imipramine, tacrine and clozapine. tha 226-233 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9868741-1 1998 The selective serotonin re-uptake inhibitor, fluvoxamine, is a very potent inhibitor of CYP1A2, and accordingly causes pharmacokinetic interactions with drugs metabolised by CYP1A2, such as caffeine, theophylline, imipramine, tacrine and clozapine. tha 226-233 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 174-180 9842955-0 1998 Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. tha 72-79 butyrylcholinesterase Homo sapiens 0-14 9842955-2 1998 OBJECTIVES: To determine the effects of cholinesterase inhibition with tacrine hydrochloride for the symptoms of Alzheimer disease in terms of cognitive performance, clinical global impression, behavior, and functional autonomy. tha 71-92 butyrylcholinesterase Homo sapiens 40-54 9842955-17 1998 CONCLUSIONS: Cholinesterase inhibition with tacrine appears to reduce deterioration in cognitive performance during the first 3 months and increase the odds of global clinical improvement. tha 44-51 butyrylcholinesterase Homo sapiens 13-27 9824956-3 1998 Two cholinesterase inhibitors, donepezil and tacrine, are labeled for use in patients with Alzheimer"s disease. tha 45-52 butyrylcholinesterase Homo sapiens 4-18 9742217-1 1998 The role of the functional architecture of the human acetylcholinesterase (HuAChE) active centre in accommodating the non-covalent inhibitors tacrine and huperzine A, or the carbamates pyridostigmine and physostigmine, was analysed using 16 mutants of residues lining the active-centre gorge. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 53-73 9813462-7 1998 Statistical significance in favor of THA versus other drugs employed was obtained in MMSE and ADAS-Cog tests in the studies carried out by Eagger et al. tha 37-40 alkylglycerone phosphate synthase Homo sapiens 94-98 9832383-3 1998 Pilocarpine (a muscarinic receptor agonist, 0.3 and 1.0 mg/kg) and tetrahydroaminoacridine (a cholinesterase inhibitor, 3.0 mg/kg) increased the power and deceased the frequency. tha 67-90 cholinesterase Oryctolagus cuniculus 94-108 9787282-7 1998 Tacrine, the first cholinesterase inhibitor to be so labeled, must be taken four times daily and is associated with hepatic toxicity. tha 0-7 butyrylcholinesterase Homo sapiens 19-33 9742217-4 1998 Studies with HuAChE mutants carrying replacements at positions 86, 133 and 337 indicate that the orientations of huperzine A and tacrine in the HuAChE complexes in solution are significantly different from those observed in X-ray structures of the corresponding complexes with Torpedo californica AChE (TcAChE). tha 129-136 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-19 9726626-10 1998 The challenge with metrifonate or tacrine resulted in 90 and 80% cholinesterase inhibition, respectively. tha 34-41 butyrylcholinesterase Rattus norvegicus 65-79 9651138-3 1998 The most common tacrine-associated adverse events were elevated liver transaminase levels [alanine aminotransferase (ALT) and, to a lesser degree, aspartate aminotransferase] and peripheral cholinergic events involving primarily the digestive system (nausea, vomiting, diarrhea, dyspepsia, anorexia, and weight loss). tha 16-23 glutamic--pyruvic transaminase Homo sapiens 91-115 9839013-3 1998 Compounds 4d-e were found to be more potent than galanthamine and tacrine in inhibiting AChE. tha 66-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-92 9778761-1 1998 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine), a reversible cholinesterase inhibitor, was effective in the treatment of Alzheimer"s disease (AD). tha 0-7 butyrylcholinesterase Rattus norvegicus 59-73 9778761-1 1998 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine), a reversible cholinesterase inhibitor, was effective in the treatment of Alzheimer"s disease (AD). tha 9-43 butyrylcholinesterase Rattus norvegicus 59-73 9772028-10 1998 The functional effects of tacrine in Alzheimer patients appeared to be related to both dose and length of cholinesterase inhibitor treatment. tha 26-33 butyrylcholinesterase Homo sapiens 106-120 9764962-0 1998 Caffeine based measures of CYP1A2 activity correlate with oral clearance of tacrine in patients with Alzheimer"s disease. tha 76-83 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 9764962-1 1998 AIMS: To study the potential utility of caffeine based probes of CYP1A2 enzyme activity in predicting the pharmokinetics of tacrine in patients with Alzheimer"s disease. tha 124-131 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 65-71 9764962-5 1998 CONCLUSIONS: These observations support a central role for CYP1A2 in the in vivo disposition of tacrine and the potential for drug interactions when tacrine treated patients receive known inducers or inhibitors of this enzyme. tha 96-103 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 59-65 9764962-5 1998 CONCLUSIONS: These observations support a central role for CYP1A2 in the in vivo disposition of tacrine and the potential for drug interactions when tacrine treated patients receive known inducers or inhibitors of this enzyme. tha 149-156 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 59-65 10327418-7 1998 Tacrine, but not indomethacin, cimetidine, or propentofylline, showed activity in inhibiting C1q secretion by IFN-gamma treated THP-1-derived macrophages. tha 0-7 complement C1q A chain Homo sapiens 93-96 10327418-7 1998 Tacrine, but not indomethacin, cimetidine, or propentofylline, showed activity in inhibiting C1q secretion by IFN-gamma treated THP-1-derived macrophages. tha 0-7 interferon gamma Homo sapiens 110-119 10327418-7 1998 Tacrine, but not indomethacin, cimetidine, or propentofylline, showed activity in inhibiting C1q secretion by IFN-gamma treated THP-1-derived macrophages. tha 0-7 GLI family zinc finger 2 Homo sapiens 128-133 9632220-0 1998 Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities. tha 47-54 butyrylcholinesterase Rattus norvegicus 71-85 9631459-0 1998 Tacrine and donepezil attenuate the neurotoxic effect of A beta(25-35) in rat PC12 cells. tha 0-7 amyloid beta precursor protein Rattus norvegicus 57-63 9631459-1 1998 The effect of the cholinesterase inhibitors tacrine and donepezil on A beta(25-35)-induced toxicity was investigated in rat pheochromocytoma PC12 cells by measuring the mitochondrial activity. tha 44-51 butyrylcholinesterase Rattus norvegicus 18-32 9631459-1 1998 The effect of the cholinesterase inhibitors tacrine and donepezil on A beta(25-35)-induced toxicity was investigated in rat pheochromocytoma PC12 cells by measuring the mitochondrial activity. tha 44-51 amyloid beta precursor protein Rattus norvegicus 69-75 9631459-2 1998 Tacrine and donepezil was found in clinical relevant concentrations (10(-7)-10(-6) M) to attenuate A beta(25-35)-induced toxicity in PC12 cells. tha 0-7 amyloid beta precursor protein Rattus norvegicus 99-105 9631459-4 1998 This study demonstrates that tacrine and donepezil can exert neuroprotective properties which might be of importance and contribute to the clinical efficacy of cholinesterase inhibitors in the treatment of Alzheimer"s disease. tha 29-36 butyrylcholinesterase Rattus norvegicus 160-174 9652334-3 1998 The aim of this study was to investigate the effects of tacrine, an acetylcholinesterase inhibitor which has been reported to have therapeutic potential in Alzheimer"s disease, on blood pressure and two vasopressor systems (sympathetic and vasopressinergic) in Beagle dogs. tha 56-63 acetylcholinesterase Canis lupus familiaris 68-88 9617749-13 1998 tetrahydroaminoacridine was associated with a several-fold increase in plasma levels of vasopressin, adrenaline and noradrenaline, but not of plasma renin. tha 0-23 arginine vasopressin Rattus norvegicus 88-99 9589388-3 1998 One of the drugs approved by the FDA is tacrine (9-amine-1,2,3,4 tetrahydroacridine; THA), a strong acetylcholinesterase (AChE) inhibitor. tha 40-47 acetylcholinesterase Mus musculus 100-120 9589388-3 1998 One of the drugs approved by the FDA is tacrine (9-amine-1,2,3,4 tetrahydroacridine; THA), a strong acetylcholinesterase (AChE) inhibitor. tha 40-47 acetylcholinesterase Mus musculus 122-126 9589388-3 1998 One of the drugs approved by the FDA is tacrine (9-amine-1,2,3,4 tetrahydroacridine; THA), a strong acetylcholinesterase (AChE) inhibitor. tha 85-88 acetylcholinesterase Mus musculus 100-120 9589388-3 1998 One of the drugs approved by the FDA is tacrine (9-amine-1,2,3,4 tetrahydroacridine; THA), a strong acetylcholinesterase (AChE) inhibitor. tha 85-88 acetylcholinesterase Mus musculus 122-126 15616667-3 1998 Currently used AChE inhibitors are tacrine, donepezil hydrochloride, rivastigmine and metrifonate. tha 35-42 acetylcholinesterase (Cartwright blood group) Homo sapiens 15-19 9676739-0 1998 Invited review: Cholinesterase inhibitors for Alzheimer"s disease therapy: from tacrine to future applications. tha 80-87 butyrylcholinesterase Homo sapiens 16-30 9617749-19 1998 Tetrahydroaminoacridine"s cardiovascular effects were completely blocked when rats were pretreated with prazosin plus vasopressin antagonist. tha 0-23 arginine vasopressin Rattus norvegicus 118-129 9617749-22 1998 The tetrahydroaminoacridine-induced reduction in heart rate appears to be due to the increase in vagal tone and plasma vasopressin. tha 4-27 arginine vasopressin Rattus norvegicus 119-130 9587921-4 1998 The present paper reports data regarding the evaluation on the activity of monoamine-oxidase A and B in murine neuroblastoma cells carried out by a radioassay upon acute or chronic treatment of cells by aluminium or tacrine. tha 216-223 monoamine oxidase A Mus musculus 75-100 9597187-2 1998 The conjunctive pharmacomodulation of huperzine A (carbobicyclic substructure) and tacrine (4-aminoquinoline substructure) led to compound 7jy, 2.5 times less active than tacrine as AChE inhibitor, but much more active than its (Z)-stereoisomer (7iy). tha 83-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 182-186 10022747-0 1998 Use of heterologously expressed human cytochrome P450 1A2 to predict tacrine-fluvoxamine drug interaction in man. tha 69-76 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 38-57 10022747-2 1998 In vitro metabolism of tacrine (a CYP1A2 probe) in the presence and absence of fluvoxamine, a CYP1A2 inhibitor, was investigated in human liver mircrosomes and with different rH-CYP. tha 23-30 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-40 10022747-2 1998 In vitro metabolism of tacrine (a CYP1A2 probe) in the presence and absence of fluvoxamine, a CYP1A2 inhibitor, was investigated in human liver mircrosomes and with different rH-CYP. tha 23-30 peptidylprolyl isomerase G Homo sapiens 34-37 10022747-4 1998 The extent of tacrine metabolism inhibition procured by fluvoxamine with rH-CYP1A2, was compared with previous results observed in man. tha 14-21 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 76-82 10022747-7 1998 Using the Km, Vmax and Ki determined with rH-CYP1A2, we calculated that fluvoxamine produced an inhibition of 1-, 2- and 4-hydroxytacrine formation rate of 91, 87 and 88%, respectively, in the range of tacrine and fluvoxamine concentrations observed in man. tha 130-137 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 45-51 9521254-2 1998 We analyzed data from a previously reported 30-week, double-blind, placebo-controlled trial of tacrine, in which APOE genotypes were determined from previously collected plasma samples. tha 95-102 apolipoprotein E Homo sapiens 113-117 9521254-9 1998 APOE genotype and gender may predict response to tacrine in patients with AD. tha 49-56 apolipoprotein E Homo sapiens 0-4 9619996-1 1998 Glucose and the acetylcholinesterase inhibitor tacrine were tested, alone and in combination, in mice of the CD-1 strain subjected to five daily shuttle-box training sessions. tha 47-54 acetylcholinesterase Mus musculus 16-36 9580877-5 1998 Tacrine inhibited bovine retinal AChE activity in a concentration-dependent manner; IC50 was fo to be 8.07 nM. tha 0-7 acetylcholinesterase Bos taurus 33-37 9771828-4 1998 By contrast, studies with AChE inhibitors--tacrine and donepezil--have been promising. tha 43-50 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-30 10375753-3 1998 RESULTS: Following intragastric gavage, Hup A, E2020, and tacrine all produced dose-dependent inhibitions of brain AChE. tha 58-65 acetylcholinesterase Rattus norvegicus 115-119 9405519-4 1997 The effects of the afferent stimulus were greatly enhanced in CA1 neurons exposed to the catalytic AChE inhibitors neostigmine, physostigmine, or 9-amino-1,2,3, 4-tetrahydro-acridine. tha 146-182 carbonic anhydrase 1 Rattus norvegicus 62-65 9405519-4 1997 The effects of the afferent stimulus were greatly enhanced in CA1 neurons exposed to the catalytic AChE inhibitors neostigmine, physostigmine, or 9-amino-1,2,3, 4-tetrahydro-acridine. tha 146-182 acetylcholinesterase Rattus norvegicus 99-103 9364455-5 1997 Repeated administration of tacrine resulted in decreased binding to high-affinity choline uptake, nicotinic and M2-muscarinic acetylcholine receptor sites in a number of cortical regions, while reductions in M1-muscarinic receptor binding were restricted to the cingulate and entorhinal cortex as well as caudate-putamen. tha 27-34 cholinergic receptor, muscarinic 2 Rattus norvegicus 112-148 9236571-7 1997 RESULTS: Compared with the placebo group, the percentage of patients receiving tacrine whose conditions improved or stabilized was significantly greater for 8 of 11 ADAS-cognitive items (word recall, word recognition, orientation, language production, comprehension, word finding, following commands, ideational praxis) and for the ADAS-noncognitive items: cooperation, delusions, and pacing. tha 79-86 alkylglycerone phosphate synthase Homo sapiens 165-169 9236571-9 1997 The previous demonstration of tacrine"s effect on global cognitive function has been extended by suggesting an association between tacrine therapy and improvements in individual cognitive and noncognitive items of the ADAS. tha 30-37 alkylglycerone phosphate synthase Homo sapiens 218-222 9236571-9 1997 The previous demonstration of tacrine"s effect on global cognitive function has been extended by suggesting an association between tacrine therapy and improvements in individual cognitive and noncognitive items of the ADAS. tha 131-138 alkylglycerone phosphate synthase Homo sapiens 218-222 9236571-10 1997 Effects of tacrine in clinical practice might be more accurately and efficiently assessed by measuring individual ADAS cognitive and noncognitive items relevant to individual patient pretreatment clinical status. tha 11-18 alkylglycerone phosphate synthase Homo sapiens 114-118 9241666-0 1997 Glutathione S-transferase theta genetic polymorphism might influence tacrine hepatotoxicity in Alzheimer"s patients. tha 69-76 glutathione S-transferase theta 1 Homo sapiens 0-31 9223063-1 1997 We evaluated the effect of a single dose of a cholinesterase inhibitor, tetrahydroaminoacridine (THA; 25 and 50 mg, orally), on attention in patients with Alzheimer"s disease (AD). tha 72-95 butyrylcholinesterase Homo sapiens 46-60 9223063-1 1997 We evaluated the effect of a single dose of a cholinesterase inhibitor, tetrahydroaminoacridine (THA; 25 and 50 mg, orally), on attention in patients with Alzheimer"s disease (AD). tha 97-100 butyrylcholinesterase Homo sapiens 46-60 9184816-2 1997 9-Amino-1,2,3,4-tetrahydroacridine (THA), an acetylcholinesterase inhibitor, significantly inhibited in vitro the ATP diphosphohydrolase activity of synaptosomes from the cerebral cortex and hippocampus of adult rats. tha 50-53 acetylcholinesterase Rattus norvegicus 59-79 9228650-2 1997 NIK-247, tacrine and E-2020 all strongly inhibited acetylcholinesterase (AChE) in human red blood cells (IC50s = 1.0 x 10(-6), 2.9 x 10(-7) and 3.7 x 10(-8) M, respectively). tha 9-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-71 9228650-2 1997 NIK-247, tacrine and E-2020 all strongly inhibited acetylcholinesterase (AChE) in human red blood cells (IC50s = 1.0 x 10(-6), 2.9 x 10(-7) and 3.7 x 10(-8) M, respectively). tha 9-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 9632220-5 1998 The doses that improved AF64A-induced memory deficit were correlated to about 25-30% (huperzine A) and less than 10% (E2020, tacrine) inhibition of acetylcholinesterase (AChE) activity in the cortex and hippocampus. tha 125-132 acetylcholinesterase Rattus norvegicus 148-168 9632220-6 1998 Huperzine A, E2020 and tacrine all produced dose-dependent inhibition of brain AChE following i.c.v. tha 23-30 acetylcholinesterase Rattus norvegicus 79-83 9632220-9 1998 Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BuChE) than it was brain AChE. tha 0-7 butyrylcholinesterase Rattus norvegicus 48-69 9632220-9 1998 Tacrine was more effective in inhibiting plasma butyrylcholinesterase (BuChE) than it was brain AChE. tha 0-7 butyrylcholinesterase Rattus norvegicus 71-76 9475630-4 1997 Conversely, the acetylcholinesterase inhibitor tacrine (0.5, 1, 2 or 3 mg/kg, i.p.) tha 47-54 acetylcholinesterase Mus musculus 16-36 9475630-7 1997 The preventing action of tacrine seems specifically related to the avoidance impairment induced by amitriptyline, since the acetylcholinesterase inhibitor did not reduce, but enhanced the avoidance impairing action of the neuroleptic chlorpromazine. tha 25-32 acetylcholinesterase Mus musculus 124-144 9475371-0 1997 Effect of tetrahydroaminoacridine, a cholinesterase inhibitor, on cognitive performance following experimental brain injury. tha 10-33 butyrylcholinesterase Rattus norvegicus 37-51 9475371-3 1997 We examined the effects of repeated postinjury administration of a cholinesterase inhibitor, tetrahydroaminoacridine (THA), on cognitive performance following experimental TBI. tha 93-116 butyrylcholinesterase Rattus norvegicus 67-81 9475371-3 1997 We examined the effects of repeated postinjury administration of a cholinesterase inhibitor, tetrahydroaminoacridine (THA), on cognitive performance following experimental TBI. tha 118-121 butyrylcholinesterase Rattus norvegicus 67-81 9469652-1 1997 Effect of tacrine, a cholinesterase inhibitor, on spatial acquisition deficit caused by permanent occlusion of bilateral common carotid arteries (2VO) was examined by using the conventional 8-arm and the 4-arm baited radial maze tasks in rats. tha 10-17 butyrylcholinesterase Rattus norvegicus 21-35 9567741-5 1997 Although cholinesterase inhibitors such as tacrine and galanthamine offer modest clinical benefits, other cholinergic agents have proved to be of limited therapeutic value. tha 43-50 butyrylcholinesterase Homo sapiens 9-23 9357518-0 1997 Novel tacrine analogues for potential use against Alzheimer"s disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. tha 6-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-112 9357518-1 1997 Several novel analogues of tacrine have been synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase, and neuronal uptake of 5-HT (serotonin) and noradrenaline. tha 27-34 acetylcholinesterase (Cartwright blood group) Homo sapiens 97-117 9357518-1 1997 Several novel analogues of tacrine have been synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase, and neuronal uptake of 5-HT (serotonin) and noradrenaline. tha 27-34 butyrylcholinesterase Homo sapiens 119-140 9357518-2 1997 Changes in the size of the carbocyclic ring of tacrine produced modest potency against cholinesterase enzymes. tha 47-54 butyrylcholinesterase Homo sapiens 87-101 15989517-3 1997 In vitro, donepezil is about 10 times more potent than tacrine as an inhibitor of acetylcholinesterase. tha 55-62 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-102 9329702-6 1997 Furthermore, among women on ERT receiving tacrine, there tended to be greater improvement relative to placebo among those without an APOE-epsilon 4 allele. tha 42-49 apolipoprotein E Homo sapiens 133-137 9342788-1 1997 The present study investigates the effects of 25 or 50 mg tetrahydroaminoacridine (THA), a cholinesterase inhibitor, on auditory mismatch negativity (MMN) event-related response in 19 patients with Alzheimer disease (AD). tha 58-81 butyrylcholinesterase Homo sapiens 91-105 9342788-1 1997 The present study investigates the effects of 25 or 50 mg tetrahydroaminoacridine (THA), a cholinesterase inhibitor, on auditory mismatch negativity (MMN) event-related response in 19 patients with Alzheimer disease (AD). tha 83-86 butyrylcholinesterase Homo sapiens 91-105 9278102-0 1997 Characterization of the induction of rat microsomal cytochrome P450 by tacrine. tha 71-78 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 52-67 9278102-1 1997 The effect of multiple-dose tacrine (THA) administration at 2 and 20 mg/kg (single oral doses for 2 weeks) on cytochrome P450 (CYP) was examined in male and female Wistar rats. tha 28-35 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 110-125 9278102-1 1997 The effect of multiple-dose tacrine (THA) administration at 2 and 20 mg/kg (single oral doses for 2 weeks) on cytochrome P450 (CYP) was examined in male and female Wistar rats. tha 28-35 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 127-130 9278102-1 1997 The effect of multiple-dose tacrine (THA) administration at 2 and 20 mg/kg (single oral doses for 2 weeks) on cytochrome P450 (CYP) was examined in male and female Wistar rats. tha 37-40 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 110-125 9278102-1 1997 The effect of multiple-dose tacrine (THA) administration at 2 and 20 mg/kg (single oral doses for 2 weeks) on cytochrome P450 (CYP) was examined in male and female Wistar rats. tha 37-40 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 127-130 9278102-5 1997 Male and female animals treated with 20 mg/kg THA for 2 weeks demonstrated increased CYP1A activity (increased ethoxyresorufin deethylase activity) and increased expression of CYP1A1 with only minor increases in CYP1A2 expression. tha 46-49 cytochrome P450, family 1, subfamily a, polypeptide 1 Rattus norvegicus 176-182 9278102-5 1997 Male and female animals treated with 20 mg/kg THA for 2 weeks demonstrated increased CYP1A activity (increased ethoxyresorufin deethylase activity) and increased expression of CYP1A1 with only minor increases in CYP1A2 expression. tha 46-49 cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus 212-218 9209244-0 1997 Influence of the CYP1A2 inhibitor fluvoxamine on tacrine pharmacokinetics in humans. tha 49-56 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 17-23 9209244-1 1997 OBJECTIVE: Tacrine is extensively metabolized by cytochrome P4501A2 (CYP1A2). tha 11-18 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 49-67 9209244-1 1997 OBJECTIVE: Tacrine is extensively metabolized by cytochrome P4501A2 (CYP1A2). tha 11-18 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 69-75 9209244-2 1997 Fluvoxamine, a potent CYP1A2 inhibitor, may be coadministered with tacrine. tha 67-74 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 22-28 9190877-4 1997 The rCBF response abolished by pretreatment with scopolamine was recovered by administration of physostigmine (1 or 10 microg/kg), E2020 (10 or 100 microg/kg) or tacrine (100 or 1000 microg/kg), in a dose-dependent manner. tha 162-169 CCAAT/enhancer binding protein zeta Rattus norvegicus 4-8 9226744-1 1997 Hepatotoxicity limits the clinical utility of the cholinesterase inhibitor tacrine as a palliative therapy for Alzheimer"s disease. tha 75-82 butyrylcholinesterase Macaca mulatta 50-64 9184816-0 1997 Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA) on ATP diphosphohydrolase (EC 3.6.1.5) and 5"-nucleotidase (EC 3.1.3.5) from rat brain synaptosomes. tha 47-50 5' nucleotidase, ecto Rattus norvegicus 95-110 9580877-6 1998 The Michaelis-Menten constant (Ka) for the hydrolysis of acetylthiocholine iodide (ASCh) by AChE was 0.061 mM in the control system, and this value was increased by 54-67% in the tacrine-treated systems. tha 179-186 acetylcholinesterase Bos taurus 92-96 9130298-2 1997 Cholinesterase inhibitors-tetrahydro-aminoacridine (THA: 1.0 and 3.0 mg/kg i.p.) tha 26-50 butyrylcholinesterase Rattus norvegicus 0-14 9130298-2 1997 Cholinesterase inhibitors-tetrahydro-aminoacridine (THA: 1.0 and 3.0 mg/kg i.p.) tha 52-55 butyrylcholinesterase Rattus norvegicus 0-14 9065319-6 1997 Treatment with the cholinesterase inhibitor tacrine (80 mg daily) during 3 months to AD patients resulted in a mean plasma concentration of 7.7 +/- 0.8 ng/ml and a corresponding inhibition of the cholinesterase activity in plasma by 34 +/- 5%. tha 44-51 butyrylcholinesterase Homo sapiens 19-33 9098680-0 1997 Tremulous jaw movements induced by the acetylcholinesterase inhibitor tacrine: effects of antiparkinsonian drugs. tha 70-77 acetylcholinesterase Rattus norvegicus 39-59 9065319-6 1997 Treatment with the cholinesterase inhibitor tacrine (80 mg daily) during 3 months to AD patients resulted in a mean plasma concentration of 7.7 +/- 0.8 ng/ml and a corresponding inhibition of the cholinesterase activity in plasma by 34 +/- 5%. tha 44-51 butyrylcholinesterase Homo sapiens 196-210 9062656-2 1997 AChE inhibitors, including physostigmine, E-2020, amiridin, tetrahydroaminoacridine (THA) and Nicergoline had a poor effect on AChE present in the senile plaque-rich fraction isolated from Alzheimer brain than that either in the soluble fraction of Alzheimer brain or in the control brain. tha 60-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 9065747-0 1997 Noninterference of cytochrome P4501A2 in the cytotoxicity of tacrine using genetically engineered V79 Chinese hamster cells for stable expression of the human or rat isoform and two human hepatocyte cell lines. tha 61-68 cytochrome P450 1A2 Cricetulus griseus 19-37 9065747-3 1997 THA-induced toxicity may be related to a metabolic pathway implicating cytochrome P450 1A2 (CYP1A2). tha 0-3 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 71-90 9065747-3 1997 THA-induced toxicity may be related to a metabolic pathway implicating cytochrome P450 1A2 (CYP1A2). tha 0-3 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 92-98 9065747-4 1997 The purpose of this study was to clarify the role of the metabolic conversion of THA by CYP1A2 in the cytotoxicity of THA. tha 81-84 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9065747-4 1997 The purpose of this study was to clarify the role of the metabolic conversion of THA by CYP1A2 in the cytotoxicity of THA. tha 118-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 88-94 9065747-5 1997 The cytotoxicity of THA was evaluated in two human hepatocyte cell lines, HepG2 and Chang liver, and on the V79 Chinese hamster cell line, which does not express cytochrome P450 activity, and its variants, genetically engineered for expression of human or rat CYP1A2. tha 20-23 cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus 260-266 9062689-5 1997 On the other hand, tetrahydroaminoacridine (THA), an acetylcholinesterase (AChE) inhibitor, increased the extracellular acetylcholine level in both regions. tha 19-42 acetylcholinesterase Rattus norvegicus 75-79 9062689-5 1997 On the other hand, tetrahydroaminoacridine (THA), an acetylcholinesterase (AChE) inhibitor, increased the extracellular acetylcholine level in both regions. tha 44-47 acetylcholinesterase Rattus norvegicus 75-79 9062656-2 1997 AChE inhibitors, including physostigmine, E-2020, amiridin, tetrahydroaminoacridine (THA) and Nicergoline had a poor effect on AChE present in the senile plaque-rich fraction isolated from Alzheimer brain than that either in the soluble fraction of Alzheimer brain or in the control brain. tha 85-88 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 9084068-4 1997 However, THA 50 mg increased alpha activity and alpha/theta ratio in -APOE4 patients. tha 9-12 apolipoprotein E Homo sapiens 70-75 9366505-0 1997 The effect of tacrine and leupeptin on the secretion of the beta-amyloid precursor protein in HeLa cells. tha 14-21 amyloid beta precursor protein Homo sapiens 60-90 9084060-10 1997 Pretreatment with mecamylamine completely blocked the THA-induced increase in NA and 5-HT turnover, but not in DA turnover, suggesting that the nACh-R system is involved in the THA-induced increase in brain NA and 5-HT turnover. tha 54-57 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 144-150 9084060-11 1997 On the other hand, (-)-cytisine, a partial agonist for the beta 2 subunit containing nACh-R, completely inhibited the nACh-R agonist- and THA-induced increases in NA turnover, but not in DA turnover, and normalized the changes in 5-HT turnover. tha 138-141 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 85-91 9084060-11 1997 On the other hand, (-)-cytisine, a partial agonist for the beta 2 subunit containing nACh-R, completely inhibited the nACh-R agonist- and THA-induced increases in NA turnover, but not in DA turnover, and normalized the changes in 5-HT turnover. tha 138-141 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 118-124 9084068-0 1997 The ability of THA treatment to increase cortical alpha waves is related to apolipoprotein E genotype of Alzheimer disease patients. tha 15-18 apolipoprotein E Homo sapiens 76-92 9030907-4 1997 Acetylcholinesterase activity of adrenal homogenates was inhibited by tacrine and physostigmine in a concentration-dependent manner. tha 70-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 9453170-1 1997 It has been suggested that tacrine (THA) induced hepatotoxicity was related to its metabolic pathway involving cytochrome P4501A2 (CYP1A2). tha 27-34 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 111-129 9453170-1 1997 It has been suggested that tacrine (THA) induced hepatotoxicity was related to its metabolic pathway involving cytochrome P4501A2 (CYP1A2). tha 27-34 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 131-137 9366505-4 1997 Tacrine, a centrally active potent cholinesterase inhibitor that has been shown to improve cognitive functions in some patients with AD, inhibits the secretion of sAPP. tha 0-7 butyrylcholinesterase Homo sapiens 35-49 8993489-0 1996 Apolipoprotein E genotype and gender influence response to tacrine therapy. tha 59-66 apolipoprotein E Homo sapiens 0-16 8978837-1 1996 The method of comparative molecular field analysis (CoMFA) was used to develop quantitative structure-activity relationships for physostigmine, 9-amino-1,2,3,4-tetrahydroacridine (THA), edrophonium (EDR), and other structurally diverse inhibitors of acetylcholinesterase (AChE). tha 144-178 acetylcholinesterase (Cartwright blood group) Homo sapiens 250-270 8993489-1 1996 Our objective is to evaluate the effects of apolipoprotein E genotype (APOE) on clinical response to treatment with tacrine, in patients with Alzheimer"s disease (AD). tha 116-123 apolipoprotein E Homo sapiens 44-60 8993489-1 1996 Our objective is to evaluate the effects of apolipoprotein E genotype (APOE) on clinical response to treatment with tacrine, in patients with Alzheimer"s disease (AD). tha 116-123 apolipoprotein E Homo sapiens 71-75 8993489-11 1996 APOE genotype may be a predictor for clinical response to tacrine in AD patients, APOE epsilon 4 associated with a lower probability of cognitive improvement. tha 58-65 apolipoprotein E Homo sapiens 0-4 8993489-11 1996 APOE genotype may be a predictor for clinical response to tacrine in AD patients, APOE epsilon 4 associated with a lower probability of cognitive improvement. tha 58-65 apolipoprotein E Homo sapiens 82-86 9035375-2 1996 The most potent analogue in our series was the 9-heptylamino-6-methoxytacrine 3af which, in comparison with tacrine (THA), displayed an almost identical inhibitory effect, slightly lower acute toxicity and higher selectivity profile towards AchE when compared with THA. tha 70-77 acetylcholinesterase (Cartwright blood group) Homo sapiens 241-245 8967962-1 1996 Butyrylcholinesterase [BuChE (acylcholine acyl hydrolase); EC 3.1.1.8] limits the access of drugs, including tacrine, to other proteins. tha 109-116 butyrylcholinesterase Homo sapiens 0-21 8960873-3 1996 The formation of the metabolite, tele-methylhistamine, in brain of mice treated with an histamine H3 receptor antagonist was abolished by tacrine with an ID50 as low as 1.2 +/- 0.4 mg/kg. tha 138-145 histamine receptor H3 Mus musculus 88-109 8937715-8 1996 The cholinesterase inhibitor, tacrine (1 microM), potentiated the effect of pentamidine; in contrast, morphine inhibited pentamidine-induced responses. tha 30-37 butyrylcholinesterase Homo sapiens 4-18 9154234-7 1996 Furthermore, protein kinase C activators (phorbol ester and 1-oleyl-2-acetyl-glycerol) and tacrine reversed A beta-induced toxicity. tha 91-98 amyloid beta precursor protein Rattus norvegicus 108-114 8858982-5 1996 However, tetrahydroaminoacridine, an acetylcholinesterase inhibitor, significantly increased the extracellular ACh level in the rat frontal cortex and weakly increased the hippocampal level. tha 9-32 acetylcholinesterase Rattus norvegicus 37-57 8798583-0 1996 Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. tha 43-63 acetylcholinesterase Rattus norvegicus 78-98 8798583-4 1996 These analogs were up to 10,000-fold more selective and 1,000-fold more potent than THA in inhibiting rat AChE and yet required one simple reaction to synthesize. tha 84-87 acetylcholinesterase Rattus norvegicus 106-110 8928167-2 1996 The authors describe the rationale for use of the acetylcholinesterase inhibitor, tacrine, in Alzheimer"s disease and critically review the controlled clinical trials using this drug. tha 82-89 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-70 8949256-6 1996 In dementia, the cholinesterase inhibitor, tacrine, produces worthwhile improvement in about 40% of patients able to tolerate adequate doses. tha 43-50 butyrylcholinesterase Homo sapiens 17-31 8731520-1 1996 The present study investigated the impact of the cholinesterase inhibitor tetrahydroaminoacridine (THA; tacrine) on sleep in healthy subjects. tha 74-97 butyrylcholinesterase Homo sapiens 49-63 8675160-2 1996 Recent studies using human liver microsomes have suggested that a single liver enzyme, cytochrome P450 1A2 (CYP1A2), catalyzes the major route of metabolism and elimination of tacrine, and also catalyzes the pathway(s) involved in the generation of reactive metabolites capable of covalent protein binding and cytotoxicity. tha 176-183 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 87-106 8675160-2 1996 Recent studies using human liver microsomes have suggested that a single liver enzyme, cytochrome P450 1A2 (CYP1A2), catalyzes the major route of metabolism and elimination of tacrine, and also catalyzes the pathway(s) involved in the generation of reactive metabolites capable of covalent protein binding and cytotoxicity. tha 176-183 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 108-114 8675160-3 1996 Because CYP1A2 activity has been shown to vary up to 60-fold among patients, we proposed that a convenient measure of CYP1A2 activity, the [(13)C 3-methyl] caffeine breath test (CBT), might be clinically useful in identifying patients most susceptible to tacrine liver toxicity. tha 255-262 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 118-124 8675160-12 1996 However, the correlation we observed between CBT results and tacrine blood levels is the first evidence supporting a critical role for CYP1A2 activity in the disposition of the drug in vivo. tha 61-68 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 135-141 8781777-2 1996 Tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA), Cognex] is a potent acetylcholinesterase inhibitor recently approved for treatment of mild-to-moderate Alzheimer"s disease. tha 0-7 acetylcholinesterase Rattus norvegicus 100-120 8781777-2 1996 Tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA), Cognex] is a potent acetylcholinesterase inhibitor recently approved for treatment of mild-to-moderate Alzheimer"s disease. tha 9-72 acetylcholinesterase Rattus norvegicus 100-120 8781777-2 1996 Tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA), Cognex] is a potent acetylcholinesterase inhibitor recently approved for treatment of mild-to-moderate Alzheimer"s disease. tha 74-77 acetylcholinesterase Rattus norvegicus 100-120 8781777-2 1996 Tacrine [1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate (THA), Cognex] is a potent acetylcholinesterase inhibitor recently approved for treatment of mild-to-moderate Alzheimer"s disease. tha 80-86 acetylcholinesterase Rattus norvegicus 100-120 8731520-1 1996 The present study investigated the impact of the cholinesterase inhibitor tetrahydroaminoacridine (THA; tacrine) on sleep in healthy subjects. tha 99-102 butyrylcholinesterase Homo sapiens 49-63 8731520-7 1996 The reversible cholinesterase inhibitor THA exerts effects on REM latency comparable to those observed with other cholinomimetic agents. tha 40-43 butyrylcholinesterase Homo sapiens 15-29 8804059-5 1996 and partially alleviated by a reference cholinesterase inhibitor, THA (3 and 6 mg kg-1, i.p.). tha 66-69 butyrylcholinesterase Rattus norvegicus 40-54 8744931-2 1996 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. tha 0-34 acetylcholinesterase Mus musculus 61-81 8744931-2 1996 9-Amino-1,2,3,4-tetrahydroacridine (THA), a centrally acting acetylcholinesterase inhibitor, was used as a model drug. tha 36-39 acetylcholinesterase Mus musculus 61-81 8866685-1 1996 The pharmacokinetics of the cholinesterase inhibitor tacrine was studied in 5 Alzheimer patients during 12-31 months of treatment. tha 53-60 butyrylcholinesterase Homo sapiens 28-42 8835781-0 1996 Differential effect of tacrine and physostigmine on the secretion of the beta-amyloid precursor protein in cell lines. tha 23-30 amyloid beta precursor protein Homo sapiens 73-103 8866685-7 1996 A significant correlation was obtained between the plasma concentration of tacrine and the inhibition of ChE activity (p < 0.001). tha 75-82 butyrylcholinesterase Homo sapiens 105-108 8785468-13 1996 The cholinomimetic drugs, especially the acetylcholinesterase inhibitor tacrine, have provided a very modest benefit, slowing the progression of the illness for a number of months. tha 72-79 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-61 9139239-8 1996 Another reference compound, tetrahydroaminoacridine (THA), also induced a reversible inhibition of rat brain and serum cholinesterase, but with a mechanism of action different from that of both dichlorvos and physostigmine in that enzyme inhibition occurred rapidly upon drug addition at an allosteric site on the enzyme surface. tha 28-51 butyrylcholinesterase Rattus norvegicus 119-133 9139239-8 1996 Another reference compound, tetrahydroaminoacridine (THA), also induced a reversible inhibition of rat brain and serum cholinesterase, but with a mechanism of action different from that of both dichlorvos and physostigmine in that enzyme inhibition occurred rapidly upon drug addition at an allosteric site on the enzyme surface. tha 53-56 butyrylcholinesterase Rattus norvegicus 119-133 8997426-6 1996 The cholinesterase inhibitor tacrine is in clinical use in many countries. tha 29-36 butyrylcholinesterase Homo sapiens 4-18 8679062-1 1996 Factor analysis methodology applied to Alzheimer"s Disease Assessment Scale (ADAS) subtest profiles for patients in two large-scale clinical trials of the antidementia drug tacrine yielded three oblique factors interpreted as dysfunctions in memory, language, and praxis. tha 173-180 alkylglycerone phosphate synthase Homo sapiens 77-81 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 85-109 acetylcholinesterase Camelus bactrianus 45-65 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 85-109 acetylcholinesterase Camelus bactrianus 67-71 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 111-114 acetylcholinesterase Camelus bactrianus 45-65 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 111-114 acetylcholinesterase Camelus bactrianus 67-71 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 116-123 acetylcholinesterase Camelus bactrianus 45-65 8951687-1 1996 The nature of the inhibition of camel retina acetylcholinesterase (AChE) activity by tetrahydro-aminoacridine (THA, tacrine) has been investigated in the present study. tha 116-123 acetylcholinesterase Camelus bactrianus 67-71 8951687-2 1996 The non-significant change of the percent inhibition of AChE by THA with respect to various lengths of the preincubation period showed the type of the reversible inhibition. tha 64-67 acetylcholinesterase Camelus bactrianus 56-60 8628110-12 1996 THA administration resulted in a significant decrease in AChE activity (p<0.001) in cortex (62% decrease), hippocampus (78% decrease), and hypothalamus (90% decrease). tha 0-3 acetylcholinesterase Rattus norvegicus 57-61 8618881-8 1995 The effect of the apoE4 allele on cholinomimetic drug responsiveness was assessed next in a group (n = 40) of AD patients who completed a double-blind, 30-week clinical trial of the cholinesterase inhibitor tacrine. tha 207-214 butyrylcholinesterase Homo sapiens 182-196 8951687-0 1996 The nature of the inhibition of camel retina acetylcholinesterase (EC 3.1.1.7) activity by tetrahydroaminoacridine. tha 91-114 acetylcholinesterase Camelus bactrianus 45-65 8761343-0 1996 Amyloidogenic processing of Alzheimer"s amyloid precursor protein in vitro and its modulation by metal ions and tacrine. tha 112-119 amyloid beta precursor protein Homo sapiens 40-65 8846227-4 1995 AChE inhibitors, physostigmine and Tacrine can slow the decline of cognitive function and memory in some patients with mild or moderate AD, if given for at least 3-6 months in sufficient doses to inhibit brain AChE. tha 35-42 acetylcholinesterase (Cartwright blood group) Homo sapiens 210-214 7482577-1 1995 The effects of 7-methoxytacrine (7-MEOTA), a less toxic derivative of tetrahydroaminoacridine, on the activity of acetylcholinesterase (AChE) molecular forms were investigated in vitro. tha 70-93 acetylcholinesterase Rattus norvegicus 114-134 7482577-1 1995 The effects of 7-methoxytacrine (7-MEOTA), a less toxic derivative of tetrahydroaminoacridine, on the activity of acetylcholinesterase (AChE) molecular forms were investigated in vitro. tha 70-93 acetylcholinesterase Rattus norvegicus 136-140 8565783-0 1995 Determination of human hepatic cytochrome P4501A2 activity in vitro use of tacrine as an isoenzyme-specific probe. tha 75-82 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 31-49 9383467-3 1995 We set out to apply this method to develop more effective analogs of the known, marketed drug tacrine, an acetylcholinesterase inhibitor. tha 94-101 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 9383467-5 1995 The resulting library of (formally) 72 tetrahydroacridines was screened against acetylcholinesterase, and a compound 10-fold more potent than tacrine, 7-nitrotacrine, was discovered. tha 142-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 80-100 8528370-4 1995 After 14 months the tacrine-treated patients showed a stable rCBF level and a significant increase in rCBF in the central-parietal regions, compared to the untreated reference group, who showed typical AD reductions in rCBF in these regions. tha 20-27 CCAAT/enhancer binding protein zeta Rattus norvegicus 61-65 8528370-4 1995 After 14 months the tacrine-treated patients showed a stable rCBF level and a significant increase in rCBF in the central-parietal regions, compared to the untreated reference group, who showed typical AD reductions in rCBF in these regions. tha 20-27 CCAAT/enhancer binding protein zeta Rattus norvegicus 102-106 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). tha 48-55 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 123-141 8528370-4 1995 After 14 months the tacrine-treated patients showed a stable rCBF level and a significant increase in rCBF in the central-parietal regions, compared to the untreated reference group, who showed typical AD reductions in rCBF in these regions. tha 20-27 CCAAT/enhancer binding protein zeta Rattus norvegicus 102-106 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). tha 48-55 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 143-149 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). tha 57-91 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 123-141 8565783-1 1995 Oxidative metabolism of the cognition activator tacrine (1,2,3,4-tetrahydro-9-aminoacridine) is thought to be catalyzed by cytochrome P4501A2 (CYP1A2). tha 57-91 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 143-149 8565783-2 1995 In this study, the use of tacrine as a specific substrate to measure CYP1A2 activity in vitro was investigated. tha 26-33 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 69-75 8565783-4 1995 Initially, the percentage conversion of tacrine to stable metabolites (i.e. 1-, 2-, 4-, and 7-hydroxytacrine) at a single time point was correlated with levels of CYP1A2 apoprotein. tha 40-47 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 163-169 8565783-14 1995 It is concluded, therefore, that tacrine is a valuable probe for the determination of human hepatic CYP1A2 activity in vitro. tha 33-40 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 100-106 7763338-5 1995 Initial efforts focused on inhibition of cholinesterase activity with tacrine (1,2,3,4-tetrahydroaminoacridine monochloride, CAS 1684-40-8, THA, Cognex). tha 70-77 butyrylcholinesterase Homo sapiens 41-55 7636741-5 1995 The purpose of this study was to determine the selectivity of physostigmine, metrifonate, methanesulfonyl fluoride and tetrahydroaminoacridine (tacrine) toward AChE as compared with butyrylcholinesterase (BChE) in human cortex. tha 119-142 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 7636741-5 1995 The purpose of this study was to determine the selectivity of physostigmine, metrifonate, methanesulfonyl fluoride and tetrahydroaminoacridine (tacrine) toward AChE as compared with butyrylcholinesterase (BChE) in human cortex. tha 144-151 acetylcholinesterase (Cartwright blood group) Homo sapiens 160-164 7636741-5 1995 The purpose of this study was to determine the selectivity of physostigmine, metrifonate, methanesulfonyl fluoride and tetrahydroaminoacridine (tacrine) toward AChE as compared with butyrylcholinesterase (BChE) in human cortex. tha 144-151 butyrylcholinesterase Homo sapiens 205-209 24283645-3 1995 The assessment of potential benefit of tacrine ("best dose") was based on demonstrating improvement on the Alzheimer"s Disease Assessment Scale (ADAS) total score versus a blinded placebo. tha 39-46 alkylglycerone phosphate synthase Homo sapiens 145-149 24283645-6 1995 Results indicated that tacrine-treated patients showed improved functioning based on the ADAS-Cognitive in comparison to placebo-treated patients. tha 23-30 alkylglycerone phosphate synthase Homo sapiens 89-93 7656503-12 1995 In vitro metabolism studies have demonstrated the importance of cytochrome P450 (CYP1A2) in the biotransformation of tacrine to 1-, 2-, 4- and 7-hydroxylated metabolites. tha 117-124 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 81-87 8545521-11 1995 Acetylcholinesterase inhibitors heptylphysostigmine, galanthamine (0.63-2.5 mg/kg, IP) and tacrine (0.63-10.0 mg/kg, IP) all enhanced the rate of decrement of olfactory investigation when administered alone, but had differential effects on aggression. tha 91-98 acetylcholinesterase Mus musculus 0-20 7586900-2 1995 It has been shown in the majority of clinical trials that cholinesterase inhibitors, such as tacrine (tetrahydroaminoacridine), are able to induce beneficial effects in cognition and memory. tha 93-100 butyrylcholinesterase Homo sapiens 58-72 7586900-2 1995 It has been shown in the majority of clinical trials that cholinesterase inhibitors, such as tacrine (tetrahydroaminoacridine), are able to induce beneficial effects in cognition and memory. tha 102-125 butyrylcholinesterase Homo sapiens 58-72 8527921-12 1995 Overall, the tacrine affinity resin which is simple and inexpensive to produce allows for the selective isolation of AChE from diverse biological matrices. tha 13-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 117-121 7669991-1 1995 We designed the present study to investigate the hypothesis that progression of hippocampal pathology may decrease the therapeutic effects of anti-cholinesterase drug, tetrahydroaminoacridine, on memory functioning in Alzheimer"s disease (AD) patients. tha 168-191 butyrylcholinesterase Homo sapiens 147-161 8519521-2 1995 A class of compounds, 9-aminoacridines, have long been known to be reversible inhibitors of acetylcholinesterase (AChE-EC 3.1.1.7), the most familiar of which is 9-amino-1,2,3,4-tetrahydroacridine (Tacrine). tha 162-196 acetylcholinesterase Mus musculus 114-118 8519521-2 1995 A class of compounds, 9-aminoacridines, have long been known to be reversible inhibitors of acetylcholinesterase (AChE-EC 3.1.1.7), the most familiar of which is 9-amino-1,2,3,4-tetrahydroacridine (Tacrine). tha 198-205 acetylcholinesterase Mus musculus 114-118 7664190-1 1995 The cholinesterase inhibitor tacrine exerts a marked therapeutic effect only at a dose which is not tolerated by many patients because of the gastrointestinal side effects and hepatotoxicity of the drug. tha 29-36 butyrylcholinesterase Homo sapiens 4-18 7640148-0 1995 Glutathione S-transferase mu genotype (GSTM1*0) in Alzheimer"s patients with tacrine transaminitis. tha 77-84 glutathione S-transferase mu 1 Homo sapiens 39-44 7640148-10 1995 The frequency of the GSTM1*0 genotype in patients with tacrine transaminitis (n = 33; 45.5%) was not significantly different from that in patients treated with tacrine without liver dysfunction (n = 37; 43%), and when compared with all the controls used in the study (n = 167; 56%). tha 55-62 glutathione S-transferase mu 1 Homo sapiens 21-26 7763338-5 1995 Initial efforts focused on inhibition of cholinesterase activity with tacrine (1,2,3,4-tetrahydroaminoacridine monochloride, CAS 1684-40-8, THA, Cognex). tha 145-151 butyrylcholinesterase Homo sapiens 41-55 7763338-6 1995 Tacrine is a mixed, reversible inhibitor of cholinesterase activity that binds near but not to the catalytically active serine in the active site of the enzyme. tha 0-7 butyrylcholinesterase Homo sapiens 44-58 8534422-4 1995 Tacrine, the first cholinesterase inhibitor to be approved for the treatment of AD, has, at best, modest effects on 20-50% of patients and is associated with a high frequency of side effects, including liver transaminitis. tha 0-7 butyrylcholinesterase Homo sapiens 19-33 8548601-7 1995 A reversible inhibitor of acetylcholinesterase, tacrine, has been approved in the United States and other countries for the symptomatic treatment of mild to moderate AD, but its use still arises many questions. tha 48-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 26-46 8570945-1 1995 The approval for marketing of tacrine (Cognex), an acetylcholinesterase inhibitor, allowed physicians and the general people to attract attention to a degenerative disease, which prevalence dramatically increases every year. tha 30-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-71 8570945-1 1995 The approval for marketing of tacrine (Cognex), an acetylcholinesterase inhibitor, allowed physicians and the general people to attract attention to a degenerative disease, which prevalence dramatically increases every year. tha 39-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 51-71 7898757-0 1994 Reversibility of the effect of tacrine on the secretion of the beta-amyloid precursor protein in cultured cells. tha 31-38 amyloid beta precursor protein Homo sapiens 63-93 7894332-7 1994 Tacrine successfully prevented the M1 and M2 receptor loss in the CA1 and CA4 hippocampal subfields. tha 0-7 carbonic anhydrase 1 Rattus norvegicus 66-69 7894332-7 1994 Tacrine successfully prevented the M1 and M2 receptor loss in the CA1 and CA4 hippocampal subfields. tha 0-7 carbonic anhydrase 4 Rattus norvegicus 74-77 7898757-5 1994 Here, cell cultures were used to examine the metabolism of beta APP by tacrine, a centrally active cholinesterase inhibitor reported to improve cognitive deficits. tha 71-78 butyrylcholinesterase Homo sapiens 99-113 7866482-7 1994 This article was to evaluate whether THA treatment induced neuropeptide alteration in DAT before and after 1 year on oral THA treatment. tha 37-40 solute carrier family 6 member 3 Homo sapiens 86-89 7848798-5 1994 Tacrine, a drug that inhibits acetylcholinesterase, has proved to have a cognitive-enhancing effect, but this is limited in time and the drug has side-effects. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-50 7866482-5 1994 Tetrahydroaminoacridine (THA, tacrine) is a centrally active reversible acetylcholinesterase inhibitor. tha 0-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 7866482-5 1994 Tetrahydroaminoacridine (THA, tacrine) is a centrally active reversible acetylcholinesterase inhibitor. tha 25-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 7866482-5 1994 Tetrahydroaminoacridine (THA, tacrine) is a centrally active reversible acetylcholinesterase inhibitor. tha 30-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 7536306-5 1994 The acetylcholinesterase inhibitor, physostigmine, exerts a similar modulatory influence on the ACh current and on its extinction, and also prevents the manifestation of the effects of amiridin and tacrine. tha 198-205 acetylcholinesterase (Cartwright blood group) Homo sapiens 4-24 7816876-4 1994 Although tacrine (0.3 and 1 mg/kg, IP), a cholinesterase inhibitor, also did not affect the learning in young rats, it slightly augmented the aging-induced learning deficit in the present task. tha 9-16 butyrylcholinesterase Rattus norvegicus 42-56 7816881-5 1994 The cholinesterase inhibitors tacrine (THA) and, to a lesser extent, physostigmine (PHYSO) and amodiaquine (AMDQ), caused an upward shift in the frequency of the resting electrocortical activity, although scopolamine significantly slowed the activity below baseline levels. tha 30-37 butyrylcholinesterase Homo sapiens 4-18 7990271-6 1994 These results indicate that a high-dose of tacrine increases cholinergic neurotransmission not only by inhibition of cholinesterase but also by increasing ACh release through an atropine-like effect, perhaps by blockade of part of the process of muscarinic autoinhibition. tha 43-50 butyrylcholinesterase Rattus norvegicus 117-131 7888087-6 1994 Based on differences from placebo in scoring, a gain of 2-12 (MMSE) or 5-6 (ADAS) in deterioration can be seen for a THA treatment of 2-3 mo duration. tha 117-120 alkylglycerone phosphate synthase Homo sapiens 76-80 7946932-2 1994 Tacrine (1,2,3,4-tetrahydro-9-aminoacridine-hydrochloride: THA) underwent metabolism in vitro by a panel (n = 12) of human liver microsomes genotyped for CYP2D6, in the presence of NADPH, to both protein-reactive and stable metabolites. tha 0-7 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 154-160 7946932-7 1994 Using cytochrome P450 isoform specific inhibitors CYP1A2 was identified as the major enzyme involved in all routes of THA metabolism. tha 118-121 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 50-56 7521234-2 1994 Tacrine is a centrally acting cholinesterase inhibitor with additional pharmacological activity on monoamine levels and ion channels. tha 0-7 butyrylcholinesterase Homo sapiens 30-44 7870192-9 1994 When ChE was inhibited locally by perfusion with physostigmine, THA (5 mg/kg) produced a transient and, at its maximum, a 1.42-fold increase in extracellular ACh concentration. tha 64-67 butyrylcholinesterase Rattus norvegicus 5-8 8079912-1 1994 Tacrine, a centrally acting cholinesterase inhibitor, may improve cognitive and functional status in patients with mild to moderate Alzheimer"s disease. tha 0-7 butyrylcholinesterase Homo sapiens 28-42 8186246-0 1994 Inhibition of cholinesterase activity by tetrahydroaminoacridine and the hemisuccinate esters of tocopherol and cholesterol. tha 41-64 butyrylcholinesterase Homo sapiens 14-28 8186246-6 1994 Such potent and synergistic inhibition of AChE suggest that TS or CS, alone and in combination with THA, may prove beneficial in the treatment of organophosphate poisoning and Alzheimer"s disease. tha 100-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 42-46 8046778-4 1994 Using cell cultures, we investigated the possibility that APP processing can be regulated by a centrally active cholinesterase inhibitor, tacrine, which has recently been shown to improve memory and cognitive functions in patients with AD. tha 138-145 butyrylcholinesterase Homo sapiens 112-126 8046778-9 1994 Tacrine treatment did not alter the level of HSP-70 in cell extracts and tacrine affected mildly the secretion of PN-1. tha 73-80 serpin family E member 2 Rattus norvegicus 114-118 8139083-12 1994 Significant differences in favor of 160 mg/d of tacrine vs placebo were observed on the CIBI (P < or = .002) and ADAS-Cog and FCCA (P < or = .001), as well as caregiver-global and quality-of-life assessments (P < or = .05). tha 48-55 alkylglycerone phosphate synthase Homo sapiens 113-117 7517882-1 1994 Central administration of galanin in the mouse dose-dependently blocked the hypothermia induced by the muscarinic receptor agonist, 2-ethyl 8-methyl-2,8-diazospiro[4,5]decan-1,3-dion hydrobromide, RS86 (minimum effective dose, MED = 3 nmol) and the acetylcholinesterase inhibitor tetrahydroaminoacridine, (MED = 3 nmol). tha 280-303 galanin and GMAP prepropeptide Mus musculus 26-33 7517882-4 1994 Glibenclamide (10 nmol) also reversed the inhibitory effects of galanin on tetrahydroaminoacridine induced hypothermia. tha 75-98 galanin and GMAP prepropeptide Mus musculus 64-71 7517882-7 1994 These studies suggest that the inhibitory effect of galanin on cholinergically mediated hypothermia induced by RS86 and tetrahydroaminoacridine may be exerted via an action at ATP-sensitive K+ channels but is unlikely to be acting directly at the site labelled by [3H]glibenclamide. tha 120-143 galanin and GMAP prepropeptide Mus musculus 52-59 8019748-19 1994 Physostigmine, neostigmine, tacrine and DFP (all at 30 microM) each produced near-total (> 96%) inhibition of AChE activity. tha 28-35 acetylcholinesterase Rattus norvegicus 113-117 27520522-1 1994 Velnacrine is an hydroxylated derivative of the acetylcholinesterase inhibitor tacrine. tha 79-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-68 8168431-2 1994 In vitro experiments showed that the primary effect of THA was direct inhibition of purified fetal bovine serum acetylcholinesterase (AChE) with a slight effect on slowing the aging rate of nerve agent-inhibited AChE. tha 55-58 acetylcholinesterase Mus musculus 112-132 8168431-2 1994 In vitro experiments showed that the primary effect of THA was direct inhibition of purified fetal bovine serum acetylcholinesterase (AChE) with a slight effect on slowing the aging rate of nerve agent-inhibited AChE. tha 55-58 acetylcholinesterase Mus musculus 134-138 8168431-2 1994 In vitro experiments showed that the primary effect of THA was direct inhibition of purified fetal bovine serum acetylcholinesterase (AChE) with a slight effect on slowing the aging rate of nerve agent-inhibited AChE. tha 55-58 acetylcholinesterase Mus musculus 212-216 7868848-1 1994 In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of the cholinesterase inhibitor tacrine (tetrahydroaminoacridine, THA) were found. tha 152-159 butyrylcholinesterase Homo sapiens 127-141 7868848-1 1994 In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of the cholinesterase inhibitor tacrine (tetrahydroaminoacridine, THA) were found. tha 161-184 butyrylcholinesterase Homo sapiens 127-141 7868848-1 1994 In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of the cholinesterase inhibitor tacrine (tetrahydroaminoacridine, THA) were found. tha 186-189 butyrylcholinesterase Homo sapiens 127-141 8306579-2 1993 The study reported above examines the efficacy and tolerability of cholinesterase inhibitors, such as tetrahydroamino acridine (THA), for the management of this pathology. tha 102-126 butyrylcholinesterase Homo sapiens 67-81 7884402-5 1994 Based on differences from placebo in scoring, a gain of 2-12 (MMSE) or 5-6 (ADAS) months in deterioration can be seen for a THA treatment of 2-3 months duration. tha 124-127 alkylglycerone phosphate synthase Homo sapiens 76-80 8306579-2 1993 The study reported above examines the efficacy and tolerability of cholinesterase inhibitors, such as tetrahydroamino acridine (THA), for the management of this pathology. tha 128-131 butyrylcholinesterase Homo sapiens 67-81 8399297-9 1993 At concentrations below 100 microM, THA+ appears to release Ca2+ selectively from the InsP3-sensitive calcium stores, since prior depletion of these stores with supramaximal doses of InsP3 abolishes this response. tha 36-40 carbonic anhydrase 2 Homo sapiens 60-63 7906947-12 1993 Long-term treatment with the cholinesterase inhibitor tacrine increase the uptake of [11C]nicotine. tha 54-61 butyrylcholinesterase Homo sapiens 29-43 8399297-10 1993 At higher THA+ concentrations (above 100 microM) Ca2+ is released non-selectively from all stores. tha 10-14 carbonic anhydrase 2 Homo sapiens 49-52 8399297-11 1993 THA+ has no effect on the Ca(2+)-ATPase activity at concentrations below 100 microM, indicating that selective THA(+)-induced Ca2+ release is not due to non-specific inhibition of the microsomal Ca2+ pumps and does not affect Ca2+ leakage. tha 111-117 carbonic anhydrase 2 Homo sapiens 126-129 8372338-6 1993 The results obtained with neurotransmitter replacement therapy, e.g. with the acetylcholinesterase inhibitor tacrine, have generally been disappointing, even if a small clinical improvement has been observed in a few selected patients. tha 109-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-98 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 0-34 butyrylcholinesterase Rattus norvegicus 62-76 8401923-14 1993 The cholinesterase inhibitor, tacrine (THA), had a potency profile similar to that of gallamine but with less selectivity. tha 30-37 butyrylcholinesterase Homo sapiens 4-18 8347124-17 1993 Enoxacin, a specific inhibitor of cytochrome P450 1A2 significantly inhibited all routes of THA metabolism. tha 92-95 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 34-53 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 0-34 butyrylcholinesterase Rattus norvegicus 78-81 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 36-39 butyrylcholinesterase Rattus norvegicus 62-76 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 36-39 butyrylcholinesterase Rattus norvegicus 78-81 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 41-48 butyrylcholinesterase Rattus norvegicus 62-76 8496822-1 1993 1,2,3,4-Tetrahydro-9-aminoacridine (THA, tacrine) is a potent cholinesterase (ChE) inhibitor which is under consideration for the treatment of Alzheimer"s disease. tha 41-48 butyrylcholinesterase Rattus norvegicus 78-81 8496822-7 1993 THA (100 microM) and physostigmine (10 microM) produced an additive effect on the extracellular concentration of ACh, and the addition of THA (10 microM) to physostigmine (1 microM) produced further inhibition of in vitro ChE activity. tha 0-3 butyrylcholinesterase Rattus norvegicus 222-225 8496822-7 1993 THA (100 microM) and physostigmine (10 microM) produced an additive effect on the extracellular concentration of ACh, and the addition of THA (10 microM) to physostigmine (1 microM) produced further inhibition of in vitro ChE activity. tha 138-141 butyrylcholinesterase Rattus norvegicus 222-225 8128832-0 1993 Effects of cholinesterase inhibitors on learning and memory in rats: a brief review with special reference to THA. tha 110-113 butyrylcholinesterase Rattus norvegicus 11-25 8490946-1 1993 OBJECTIVE: Tacrine was used as a tool to examine whether block of inward rectifying potassium current (IK1) represents a mechanism for suppression of arrhythmias induced by ischaemia and reperfusion. tha 11-18 potassium calcium-activated channel subfamily N member 4 Rattus norvegicus 103-106 8490946-11 1993 CONCLUSIONS: The novel antiarrhythmic effects of tacrine, a drug with established blocking action on IK, IK1, and slow inward current, appear to result from QT widening in the rat (dependent partly on IK1 blockade in the ventricles and partly on drug induced sinus bradycardia). tha 49-56 potassium calcium-activated channel subfamily N member 4 Rattus norvegicus 105-108 8490946-11 1993 CONCLUSIONS: The novel antiarrhythmic effects of tacrine, a drug with established blocking action on IK, IK1, and slow inward current, appear to result from QT widening in the rat (dependent partly on IK1 blockade in the ventricles and partly on drug induced sinus bradycardia). tha 49-56 potassium calcium-activated channel subfamily N member 4 Rattus norvegicus 201-204 7907455-1 1993 Cholinesterase inhibitors, such as physostigmine and tacrine, have lately gained interest as potential drugs in the treatment of Alzheimer"s disease. tha 53-60 butyrylcholinesterase Homo sapiens 0-14 8466656-1 1993 The acetylcholinesterase inhibitor tetrahydroaminoacridine (THA) is known to interact with neurotransmitter systems other than the cholinergic, e.g. several studies have shown interaction of THA with the N-methyl-D-aspartate (NMDA) receptor subtype of the glutamatergic system. tha 35-58 acetylcholinesterase Rattus norvegicus 4-24 8466656-1 1993 The acetylcholinesterase inhibitor tetrahydroaminoacridine (THA) is known to interact with neurotransmitter systems other than the cholinergic, e.g. several studies have shown interaction of THA with the N-methyl-D-aspartate (NMDA) receptor subtype of the glutamatergic system. tha 60-63 acetylcholinesterase Rattus norvegicus 4-24 8466656-1 1993 The acetylcholinesterase inhibitor tetrahydroaminoacridine (THA) is known to interact with neurotransmitter systems other than the cholinergic, e.g. several studies have shown interaction of THA with the N-methyl-D-aspartate (NMDA) receptor subtype of the glutamatergic system. tha 191-194 acetylcholinesterase Rattus norvegicus 4-24 8128835-1 1993 A placebo-controlled cross-over trial (n = 89) investigated the use of a chronic dose of the cholinesterase inhibitor THA, as a treatment for dementia of the Alzheimer type (DAT). tha 118-121 butyrylcholinesterase Homo sapiens 93-107 8128835-1 1993 A placebo-controlled cross-over trial (n = 89) investigated the use of a chronic dose of the cholinesterase inhibitor THA, as a treatment for dementia of the Alzheimer type (DAT). tha 118-121 solute carrier family 6 member 3 Homo sapiens 174-177 8128838-2 1993 Special attention is paid to cholinesterase inhibitors, particularly tacrine, the drug recently approved by the FDA. tha 69-76 butyrylcholinesterase Homo sapiens 29-43 8421706-2 1993 We previously reported that traditional acetylcholinesterase inhibitors such as BW284C51, tacrine, and physostigmine were more potent inhibitors of the acetylcholinesterase in normal axons and cell bodies than of the acetylcholinesterase in plaques and tangles. tha 90-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 40-60 8421706-2 1993 We previously reported that traditional acetylcholinesterase inhibitors such as BW284C51, tacrine, and physostigmine were more potent inhibitors of the acetylcholinesterase in normal axons and cell bodies than of the acetylcholinesterase in plaques and tangles. tha 90-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 152-172 8421706-2 1993 We previously reported that traditional acetylcholinesterase inhibitors such as BW284C51, tacrine, and physostigmine were more potent inhibitors of the acetylcholinesterase in normal axons and cell bodies than of the acetylcholinesterase in plaques and tangles. tha 90-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 152-172 8358507-6 1993 The responders showed significant improvement on Digit Span, Trail Making B, and on both Clock Setting and Clock Recognition tests after 50 mg of THA. tha 146-149 TNF superfamily member 10 Homo sapiens 61-66 8128840-1 1993 This paper reviews the side effects of the two long acting cholinesterase inhibitors tacrine and velnacrine. tha 85-92 butyrylcholinesterase Homo sapiens 59-73 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 52-55 butyrylcholinesterase Rattus norvegicus 129-150 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 52-55 butyrylcholinesterase Rattus norvegicus 152-157 8371630-4 1993 The results of the present study also established that the three molecular forms of BuChE (G1, G2 and G4), recently described to be present in brain microvessels, are inhibited after THA treatment. tha 183-186 butyrylcholinesterase Rattus norvegicus 84-89 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 27-50 acetylcholinesterase Rattus norvegicus 97-117 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 27-50 acetylcholinesterase Rattus norvegicus 119-123 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 27-50 butyrylcholinesterase Rattus norvegicus 129-150 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 27-50 butyrylcholinesterase Rattus norvegicus 152-157 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 52-55 acetylcholinesterase Rattus norvegicus 97-117 8371630-1 1993 In rat brain microvessels, tetrahydroaminoacridine (THA) caused a significant inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities, in a dose-dependent manner. tha 52-55 acetylcholinesterase Rattus norvegicus 119-123 8128843-2 1993 In this study positron emission tomography (PET) was used to investigate how long-term treatment with cholinesterase inhibitors like tacrine could induce changes in the functional activity of Alzheimer brains. tha 133-140 butyrylcholinesterase Homo sapiens 102-116 8248532-0 1993 What have we learned from the THA trials to facilitate testing of new AChE inhibitors. tha 30-33 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 7870908-1 1993 Results of a placebo controlled cross-over trial (N = 89) of the anticholinesterase drug THA as a treatment for dementia of the Alzheimer"s type (DAT) are reported, with reference to previous trials of the drug and the cholinergic hypothesis of aging and dementia. tha 89-92 solute carrier family 6 member 3 Homo sapiens 146-149 8165433-4 1993 Inhibition of acetylcholinesterase in the frontal cortex and blood only was observed following administration of tacrine derivatives. tha 113-120 acetylcholinesterase Rattus norvegicus 14-34 7871003-6 1993 However, the AChE inhibitors, tetrahydroaminoacridine (THA) and physostigmine (PHY) attenuated both PCA- and SCOP-induced amnesia when administered immediately after the training session. tha 55-58 acetylcholinesterase Mus musculus 13-17 1436122-7 1992 In contrast, when ChE activity was inhibited by 10(-6) M tacrine or pretreatment with 10(-4) M DFP, the ACh overflow was partially Ca(2+)-dependent and was reduced by tetrodotoxine. tha 57-64 butyrylcholinesterase Gallus gallus 18-21 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. tha 67-101 histamine N-methyltransferase Rattus norvegicus 14-43 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. tha 67-101 histamine N-methyltransferase Rattus norvegicus 45-49 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. tha 103-110 histamine N-methyltransferase Rattus norvegicus 14-43 1530666-0 1992 Inhibition of histamine-N-methyltransferase (HNMT) by fragments of 9-amino-1,2,3,4-tetrahydroacridine (tacrine) and by beta-carbolines. tha 103-110 histamine N-methyltransferase Rattus norvegicus 45-49 1530666-1 1992 Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). tha 126-160 histamine N-methyltransferase Rattus norvegicus 0-29 8450938-1 1993 Cholinesterase inhibitors, such as physostigmine and tetrahydroaminoacridine, have been found to alleviate some of the memory deficits characteristic of senile dementia of the Alzheimer"s type (SDAT). tha 53-76 butyrylcholinesterase Rattus norvegicus 0-14 1491741-1 1992 Three patients with Alzheimer"s disease, a 68-year-old woman with mild dementia and 2 men (aged 64 and 72 years) with moderate dementia were treated orally with the cholinesterase inhibitor tacrine (tetrahydroaminoacridine), 80 mg daily, for several months. tha 190-197 butyrylcholinesterase Homo sapiens 165-179 1406817-4 1992 We conducted a multicenter trial to evaluate whether the cholinesterase inhibitor tacrine (1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate) could improve cognition in patients with Alzheimer"s disease. tha 82-89 butyrylcholinesterase Homo sapiens 57-71 1406817-4 1992 We conducted a multicenter trial to evaluate whether the cholinesterase inhibitor tacrine (1,2,3,4-tetrahydro-9-acridinamine monohydrochloride monohydrate) could improve cognition in patients with Alzheimer"s disease. tha 91-154 butyrylcholinesterase Homo sapiens 57-71 1434136-5 1992 Cholinesterase inhibitors such as tetrahydroaminoacridine (1 and 10 mg/kg, p.o. tha 34-57 butyrylcholinesterase Mus musculus 0-14 1528356-6 1992 Other drugs such as physostigmine, echothiophate, BW284C51, tetrahydroaminoacridine, and metrifonate inhibited both aqueous- and detergent-soluble AChE molecular forms with similar potency. tha 60-83 acetylcholinesterase Rattus norvegicus 147-151 1926583-2 1991 Such reversible inhibitors as tacrine (of non-competition action), ambenonium (mixed action) and galanthamine (competitive type of action) decelerate the decarbamylation rate of acetylcholinesterase. tha 30-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 178-198 1530666-1 1992 Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). tha 126-160 histamine N-methyltransferase Rattus norvegicus 31-35 1530666-1 1992 Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). tha 162-169 histamine N-methyltransferase Rattus norvegicus 0-29 1530666-1 1992 Histamine-N-methyltransferase (HNMT), the major enzyme for the metabolism of histamine in rat brain, is potently inhibited by 9-amino-1,2,3,4-tetrahydroacridine (tacrine). tha 162-169 histamine N-methyltransferase Rattus norvegicus 31-35 1530666-2 1992 Structural fragments of tacrine were less potent inhibitors of rat brain HNMT than was tacrine itself. tha 24-31 histamine N-methyltransferase Rattus norvegicus 73-77 1684233-0 1991 Somatostatin and cognitive functions in Alzheimer"s disease--the relationship of cerebrospinal fluid somatostatin increase with clinical response to tetrahydroaminoacridine. tha 149-172 somatostatin Homo sapiens 0-12 1684233-0 1991 Somatostatin and cognitive functions in Alzheimer"s disease--the relationship of cerebrospinal fluid somatostatin increase with clinical response to tetrahydroaminoacridine. tha 149-172 somatostatin Homo sapiens 101-113 1684233-1 1991 We studied the effect of tetrahydroaminoacridine (THA) on cerebrospinal fluid somatostatin-like immunoreactivity (CSF-SLI) in probable Alzheimer disease (AD) patients (n = 20) who took part in an open THA treatment trial. tha 25-48 somatostatin Homo sapiens 78-90 1684233-1 1991 We studied the effect of tetrahydroaminoacridine (THA) on cerebrospinal fluid somatostatin-like immunoreactivity (CSF-SLI) in probable Alzheimer disease (AD) patients (n = 20) who took part in an open THA treatment trial. tha 50-53 somatostatin Homo sapiens 78-90 1611059-0 1992 [Effects of amiridin and tacrine, drugs effective in Alzheimer"s disease, on the activity of monoamine oxidase A and B]. tha 25-32 monoamine oxidase A Rattus norvegicus 93-112 1611059-5 1992 Tacrine inhibited MAO-A activity at 5 x 10(-4) M concentration. tha 0-7 monoamine oxidase A Rattus norvegicus 18-23 1538717-0 1992 Interaction of tetrahydroaminoacridine with acetylcholinesterase and butyrylcholinesterase. tha 15-38 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-64 1538717-0 1992 Interaction of tetrahydroaminoacridine with acetylcholinesterase and butyrylcholinesterase. tha 15-38 butyrylcholinesterase Homo sapiens 69-90 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 99-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-54 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 99-122 acetylcholinesterase (Cartwright blood group) Homo sapiens 56-60 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 99-122 butyrylcholinesterase Homo sapiens 66-87 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 99-122 butyrylcholinesterase Homo sapiens 89-94 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 124-127 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-54 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 124-127 acetylcholinesterase (Cartwright blood group) Homo sapiens 56-60 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 124-127 butyrylcholinesterase Homo sapiens 66-87 1538717-1 1992 This paper examines inhibition of acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) by tetrahydroaminoacridine (THA), an acridine analog under consideration for palliative treatment of Alzheimer"s dementia. tha 124-127 butyrylcholinesterase Homo sapiens 89-94 1538717-2 1992 THA causes linear mixed inhibition of AchE hydrolysis of acetylthiocholine, a cationic substrate (KI = 3.8 x 10(-9) M), and linear competitive inhibition of AchE hydrolysis of 7-acetoxy-4-methylcoumarin, an uncharged substrate (KI = 6.8 x 10(-9) M), and N-methyl-7-dimethylcarbamoxyquinolinium, a cationic carbamate (KI = 1.5 x 10(-8) M). tha 0-3 acetylcholinesterase (Cartwright blood group) Homo sapiens 38-42 1538717-2 1992 THA causes linear mixed inhibition of AchE hydrolysis of acetylthiocholine, a cationic substrate (KI = 3.8 x 10(-9) M), and linear competitive inhibition of AchE hydrolysis of 7-acetoxy-4-methylcoumarin, an uncharged substrate (KI = 6.8 x 10(-9) M), and N-methyl-7-dimethylcarbamoxyquinolinium, a cationic carbamate (KI = 1.5 x 10(-8) M). tha 0-3 acetylcholinesterase (Cartwright blood group) Homo sapiens 157-161 1538717-3 1992 Propidium association with AchE in the presence of saturating concentrations of THA is characterized by a dissociation constant of 7.7 +/- 0.7 x 10(-6) M, a value within 2-fold of the dissociation constant in the absence of THA. tha 80-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 27-31 1538717-4 1992 Association of THA with AchE is, therefore, not mutually exclusive with association of propidium at the peripheral anionic site. tha 15-18 acetylcholinesterase (Cartwright blood group) Homo sapiens 24-28 1538717-5 1992 Moreover, THA causes dissociation of decidium complexes with AchE at concentrations compatible with a dissociation constant of 7.0 +/- 0.4 x 10(-9) M. Similar relationships were observed for THA inhibition of BuchE hydrolysis of butyrylthiocholine (KI = 2.5 x 10(-8) M) and dissociation of decidium complexes with BuchE (KD = 1.9 +/- 0.1 x 10(-8) M). tha 10-13 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 1538717-5 1992 Moreover, THA causes dissociation of decidium complexes with AchE at concentrations compatible with a dissociation constant of 7.0 +/- 0.4 x 10(-9) M. Similar relationships were observed for THA inhibition of BuchE hydrolysis of butyrylthiocholine (KI = 2.5 x 10(-8) M) and dissociation of decidium complexes with BuchE (KD = 1.9 +/- 0.1 x 10(-8) M). tha 10-13 butyrylcholinesterase Homo sapiens 209-214 1538717-5 1992 Moreover, THA causes dissociation of decidium complexes with AchE at concentrations compatible with a dissociation constant of 7.0 +/- 0.4 x 10(-9) M. Similar relationships were observed for THA inhibition of BuchE hydrolysis of butyrylthiocholine (KI = 2.5 x 10(-8) M) and dissociation of decidium complexes with BuchE (KD = 1.9 +/- 0.1 x 10(-8) M). tha 10-13 butyrylcholinesterase Homo sapiens 314-319 1738791-2 1992 Tacrine or galanthamine, inhibitors of acetylcholinesterase, given in conjunction with scopolamine partially reversed the scopolamine-induced deficit in passive avoidance performance. tha 0-7 acetylcholinesterase Rattus norvegicus 39-59 1761401-2 1991 THA (Tacrine), a drug used in the experimental therapy of dementia of Alzheimer"s disease type, and whose biochemical site of action is believed to be the neural cholinesterase, is shown, for the first time, to be an immunosuppressant in vitro on normal human peripheral blood lymphocytes in microgram quantities. tha 0-3 butyrylcholinesterase Homo sapiens 162-176 1761401-2 1991 THA (Tacrine), a drug used in the experimental therapy of dementia of Alzheimer"s disease type, and whose biochemical site of action is believed to be the neural cholinesterase, is shown, for the first time, to be an immunosuppressant in vitro on normal human peripheral blood lymphocytes in microgram quantities. tha 5-12 butyrylcholinesterase Homo sapiens 162-176 1954303-0 1991 Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine. tha 118-125 acetylcholinesterase (Cartwright blood group) Homo sapiens 14-34 1954303-1 1991 Galanthamine, physostigmine and 9-amino-1,2,3,4-tetrahydroacridine (tacrine) were evaluated as inhibitors of human acetylcholinesterase activity from samples of postmortem human brain, fresh brain cortex biopsies and human erythrocytes. tha 32-66 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-135 1954303-2 1991 Acetylcholinesterase activity was most effectively inhibited in all tissues by physostigmine, followed by tacrine and galanthamine. tha 106-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 1954303-5 1991 While physostigmine and tacrine acted equally on acetylcholinesterase from different sources, galanthamine was 10-fold less potent in inhibiting the enzyme activity from human brain that from human erythrocytes. tha 24-31 acetylcholinesterase (Cartwright blood group) Homo sapiens 49-69 1946590-1 1991 An in vitro comparison demonstrated that the concentration of NIK-247 that inhibited cholinesterase (ChE) activities to half the normal level (ID50) was 1.3 x 10(-6) M. This value was higher than those for both physostigmine (PHY; 1.2 x 10(-7) M) and tetrahydroaminoacridine (THA; 3.6 x 10(-7) M), which are used as cholinesterase inhibitors in the treatment of cholinergic deficits. tha 276-279 butyrylcholinesterase Rattus norvegicus 101-104 1926583-3 1991 At pH 6 tacrine inhibits the reduction rate of soluble acetylcholinesterase activity of human erythrocytes more intensively than that of membrane-bound acetylcholinesterase. tha 8-15 acetylcholinesterase (Cartwright blood group) Homo sapiens 55-75 1926583-5 1991 Tacrine, a non-competitive inhibitor in concentrations below the inhibition constant (Ki = 1.4 x 10(-7) M) exerts the most intensive effect on the decarbamylation rate of methyl- and dimethylcarbamylated acetylcholinesterase of the mouse brain, while ambenonium and galanthamine in concentrations much (tens times) exceeding their Ki (3.1 x 10(-10) M and 4.4 x 10(-7) M, respectively) provide a decrease of the decarbamylation rate. tha 0-7 acetylcholinesterase Mus musculus 204-224 1886293-0 1991 9-Amino-1,2,3,4-tetrahydroacridine is a potent inhibitor of histamine N-methyltransferase. tha 0-34 histamine N-methyltransferase Mus musculus 60-89 1886293-1 1991 The effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on histamine N-methyltransferase (HMT), an enzyme catalyzing the methylation of histamine to form tele-methylhistamine in the brain, was studied in vitro using a partially purified enzyme preparation from bovine brain and in vivo in the mouse brain. tha 14-48 histamine N-methyltransferase Bos taurus 58-87 1886293-1 1991 The effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on histamine N-methyltransferase (HMT), an enzyme catalyzing the methylation of histamine to form tele-methylhistamine in the brain, was studied in vitro using a partially purified enzyme preparation from bovine brain and in vivo in the mouse brain. tha 14-48 histamine N-methyltransferase Bos taurus 89-92 1886293-1 1991 The effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on histamine N-methyltransferase (HMT), an enzyme catalyzing the methylation of histamine to form tele-methylhistamine in the brain, was studied in vitro using a partially purified enzyme preparation from bovine brain and in vivo in the mouse brain. tha 50-53 histamine N-methyltransferase Bos taurus 58-87 1886293-1 1991 The effect of 9-amino-1,2,3,4-tetrahydroacridine (THA) on histamine N-methyltransferase (HMT), an enzyme catalyzing the methylation of histamine to form tele-methylhistamine in the brain, was studied in vitro using a partially purified enzyme preparation from bovine brain and in vivo in the mouse brain. tha 50-53 histamine N-methyltransferase Bos taurus 89-92 1886293-2 1991 THA inhibited the HMT activity in competitive and non-competitive mixed type manners with respect to histamine. tha 0-3 histamine N-methyltransferase Mus musculus 18-21 1886293-4 1991 The IC50 values for THA, 9-aminoacridine and physostigmine in the inhibition of HMT determined at fixed concentrations of histamine (20 microM) and S-adenosylmethionine (50 microM) were 0.2, 0.37 and 20 microM, respectively. tha 20-23 histamine N-methyltransferase Mus musculus 80-83 1886293-7 1991 The inhibition of HMT by THA (10 mg/kg) was marked at 30 and 60 min after treatment, but disappeared by 120 min after. tha 25-28 histamine N-methyltransferase Mus musculus 18-21 1886293-9 1991 These results indicate that THA is a potent inhibitor of HMT. tha 28-31 histamine N-methyltransferase Mus musculus 57-60 1953352-6 1991 In separate experiments, the time-course of acetylcholinesterase (AChE; EC 3.1.1.7) activity recovery was evaluated in the whole brain and diaphragm tissues of mice pretreated with THA (5 mg/kg) and physostigmine (0.1 mg/kg) 15 min before poisoning with DFP (8 mg/kg). tha 181-184 acetylcholinesterase Mus musculus 44-64 2259472-0 1990 Reversibility of the inhibition of acetylcholinesterase by tacrine. tha 59-66 acetylcholinesterase Bos taurus 35-55 2259472-1 1990 Inhibition of bovine erythrocyte acetylcholinesterase (AChE) by 1,2,3,4-tetrahydro-9-acridinamine (tacrine) was independent of time of incubation and was partially reversed by dilution and by increased substrate concentration. tha 64-97 acetylcholinesterase Bos taurus 33-53 2259472-1 1990 Inhibition of bovine erythrocyte acetylcholinesterase (AChE) by 1,2,3,4-tetrahydro-9-acridinamine (tacrine) was independent of time of incubation and was partially reversed by dilution and by increased substrate concentration. tha 64-97 acetylcholinesterase Bos taurus 55-59 2259472-1 1990 Inhibition of bovine erythrocyte acetylcholinesterase (AChE) by 1,2,3,4-tetrahydro-9-acridinamine (tacrine) was independent of time of incubation and was partially reversed by dilution and by increased substrate concentration. tha 99-106 acetylcholinesterase Bos taurus 33-53 2259472-1 1990 Inhibition of bovine erythrocyte acetylcholinesterase (AChE) by 1,2,3,4-tetrahydro-9-acridinamine (tacrine) was independent of time of incubation and was partially reversed by dilution and by increased substrate concentration. tha 99-106 acetylcholinesterase Bos taurus 55-59 1711162-2 1990 Acute tetrahydroaminoacridine (THA) dosing caused lower brain (68%) and higher plasma (90%) ChE inhibition than the other drugs studied and increased levels of brain dihydroxyphenylacetic acid (DOPAC) (236%), homovanillic acid (HVA) (197%) and 5-hydroxyindoleacetic acid (5-HIAA) (130%). tha 6-29 butyrylcholinesterase Rattus norvegicus 92-95 1711162-2 1990 Acute tetrahydroaminoacridine (THA) dosing caused lower brain (68%) and higher plasma (90%) ChE inhibition than the other drugs studied and increased levels of brain dihydroxyphenylacetic acid (DOPAC) (236%), homovanillic acid (HVA) (197%) and 5-hydroxyindoleacetic acid (5-HIAA) (130%). tha 31-34 butyrylcholinesterase Rattus norvegicus 92-95 1953352-6 1991 In separate experiments, the time-course of acetylcholinesterase (AChE; EC 3.1.1.7) activity recovery was evaluated in the whole brain and diaphragm tissues of mice pretreated with THA (5 mg/kg) and physostigmine (0.1 mg/kg) 15 min before poisoning with DFP (8 mg/kg). tha 181-184 acetylcholinesterase Mus musculus 66-70 1953352-8 1991 At 24 h after poisoning, brain AChE activity averaged 34 and 47% of that in controls in the mice protected by THA and physostigmine, respectively. tha 110-113 acetylcholinesterase Mus musculus 31-35 2390104-0 1990 Pharmacological significance of acetylcholinesterase inhibition by tetrahydroaminoacridine. tha 67-90 acetylcholinesterase Bos taurus 32-52 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 0-23 acetylcholinesterase Bos taurus 101-121 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 0-23 acetylcholinesterase Bos taurus 123-127 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 25-28 acetylcholinesterase Bos taurus 101-121 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 25-28 acetylcholinesterase Bos taurus 123-127 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 30-37 acetylcholinesterase Bos taurus 101-121 2390104-1 1990 Tetrahydroaminoacridine (THA; Tacrine) is a potent, non-competitive inhibitor of the neuronal enzyme acetylcholinesterase (AChE) and, consequently, a potent modulator of central cholinergic function. tha 30-37 acetylcholinesterase Bos taurus 123-127 2351210-1 1990 We administered tetrahydroaminoacridine (THA), a cholinesterase inhibitor, to rats with bilateral nucleus basalis magnocellularis lesions and measured their performance in a spatial learning task. tha 16-39 butyrylcholinesterase Rattus norvegicus 49-63 2403387-0 1990 Inhibition of rat brain histamine-N-methyltransferase by 9-amino-1,2,3,4-tetrahydroacridine (THA). tha 57-91 histamine N-methyltransferase Rattus norvegicus 24-53 2403387-0 1990 Inhibition of rat brain histamine-N-methyltransferase by 9-amino-1,2,3,4-tetrahydroacridine (THA). tha 93-96 histamine N-methyltransferase Rattus norvegicus 24-53 2403387-2 1990 THA shares structural features with aminoquinoline compounds known to be inhibitors of histamine-N-methyltransferase (HNMT). tha 0-3 histamine N-methyltransferase Rattus norvegicus 87-116 2403387-2 1990 THA shares structural features with aminoquinoline compounds known to be inhibitors of histamine-N-methyltransferase (HNMT). tha 0-3 histamine N-methyltransferase Rattus norvegicus 118-122 2403387-3 1990 THA was found to be a potent competitive inhibitor of rat brain HNMT in vitro, with a Ki of 35 nM with respect to both histamine and S-adenosyl-L-methionine, the co-substrate. tha 0-3 histamine N-methyltransferase Rattus norvegicus 64-68 2351210-1 1990 We administered tetrahydroaminoacridine (THA), a cholinesterase inhibitor, to rats with bilateral nucleus basalis magnocellularis lesions and measured their performance in a spatial learning task. tha 41-44 butyrylcholinesterase Rattus norvegicus 49-63 2167274-0 1990 Spin-labelling studies of the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA), a proposed drug for the treatment of Alzheimer"s disease, with erythrocyte membranes. tha 45-79 spindlin 1 Homo sapiens 0-4 2167274-0 1990 Spin-labelling studies of the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA), a proposed drug for the treatment of Alzheimer"s disease, with erythrocyte membranes. tha 81-84 spindlin 1 Homo sapiens 0-4 2167274-1 1990 ESR spin labels specific for skeletal proteins or cell-surface sialic acid have been used to monitor the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA) and its structural analogs with human erythrocyte membranes. tha 120-154 spindlin 1 Homo sapiens 4-8 2167274-1 1990 ESR spin labels specific for skeletal proteins or cell-surface sialic acid have been used to monitor the interaction of 9-amino-1,2,3,4-tetrahydroacridine (THA) and its structural analogs with human erythrocyte membranes. tha 156-159 spindlin 1 Homo sapiens 4-8 33939923-4 2021 We examined the interplay between aging and the response to tacrine-induced acetylcholinesterase inhibition, a well-characterized therapeutic treatment against dementia. tha 60-67 acetylcholinesterase Mus musculus 76-96 20504646-1 1990 The effects of a chronic treatment (21 days) with the acetylcholinesterase (AChE) inhibitor tetrahydroaminoacridine (THA) on muscarinic receptors subtypes were investigated at various times after the last administration of the drug, in various brain areas including cortex, striatum, hippocampus and cerebellum. tha 92-115 acetylcholinesterase Rattus norvegicus 54-74 20504646-1 1990 The effects of a chronic treatment (21 days) with the acetylcholinesterase (AChE) inhibitor tetrahydroaminoacridine (THA) on muscarinic receptors subtypes were investigated at various times after the last administration of the drug, in various brain areas including cortex, striatum, hippocampus and cerebellum. tha 92-115 acetylcholinesterase Rattus norvegicus 76-80 34964643-2 2022 The effect of FIB on the therapeutic potency of four FDA-approved Alzheimer"s disease drugs, namely, tacrine (TAC), donepezil (DON), eserine (ESE), and huperzine (HUP), was investigated through a combination of different in vitro and in silico experiments. tha 101-108 fibrinogen beta chain Homo sapiens 14-17 34932310-2 2022 We used matrix-assisted laser desorption/ionization mass spectrometry imaging in combination with multivariate analysis to visualize in anatomical detail metabolic effects of aging and tacrine-mediated acetylcholinesterase inhibition on comprehensive neurotransmitter systems in multiple mouse brain regions of 12-week-old and 14-month-old mice. tha 185-192 acetylcholinesterase Mus musculus 202-222 34964643-2 2022 The effect of FIB on the therapeutic potency of four FDA-approved Alzheimer"s disease drugs, namely, tacrine (TAC), donepezil (DON), eserine (ESE), and huperzine (HUP), was investigated through a combination of different in vitro and in silico experiments. tha 110-113 fibrinogen beta chain Homo sapiens 14-17 34801945-0 2022 Design, Synthesis, biological investigations and molecular interactions of triazole linked tacrine glycoconjugates as Acetylcholinesterase inhibitors with reduced hepatotoxicity. tha 91-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 34801945-1 2022 Tacrine is a known Acetylcholinesterase (AChE) inhibitors having hepatotoxicity as main liability associated with it. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 19-39 34801945-1 2022 Tacrine is a known Acetylcholinesterase (AChE) inhibitors having hepatotoxicity as main liability associated with it. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 41-45 34364052-0 2021 Synthesis, molecular docking and molecular dynamics studies of novel tacrine-carbamate derivatives as potent cholinesterase inhibitors. tha 69-76 butyrylcholinesterase Homo sapiens 109-123 34801945-3 2022 A series of triazole based glycoconjugates containing both acetylated (A-1 to A-7) and free sugar hydroxyl groups (A-8 to A-14) at the amino position of tacrine were synthesized in good yield taking aid from molecular docking studies and evaluated for their in vitro AChE inhibition activity as well as hepatotoxicity. tha 153-160 immunoglobulin kappa variable 6D-41 (non-functional) Homo sapiens 122-126 34801945-3 2022 A series of triazole based glycoconjugates containing both acetylated (A-1 to A-7) and free sugar hydroxyl groups (A-8 to A-14) at the amino position of tacrine were synthesized in good yield taking aid from molecular docking studies and evaluated for their in vitro AChE inhibition activity as well as hepatotoxicity. tha 153-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 267-271 34530383-0 2021 A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. tha 2-9 acetylcholinesterase Mus musculus 60-80 34294013-0 2021 Development of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase. tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 88-108 34294013-2 2021 The multivalent inhibition potencies for the tacrine clusters were investigated for the inhibition of acetylcholinesterase. tha 45-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 102-122 34880083-0 2021 Correction to "Tacrine Induces Endoplasmic Reticulum-Stressed Apoptosis via Disrupting the Proper Assembly of Oligomeric Acetylcholinesterase in Cultured Neuronal Cells". tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-141 34825629-0 2021 Computational design of new tacrine analogs: an in silico prediction of their cholinesterase inhibitory, antioxidant, and hepatotoxic activities. tha 28-35 butyrylcholinesterase Homo sapiens 78-92 34825629-1 2021 Tacrine, the first drug approved for the treatment of Alzheimer"s disease (AD), is a non-competitive cholinesterase inhibitor withdrawn due to its acute hepatotoxicity. tha 0-7 butyrylcholinesterase Homo sapiens 101-115 34825629-6 2021 As a result, six new tacrine analogs have been proposed as potential inhibitors of cholinesterase with antioxidant activity and low or no hepatotoxicity. tha 21-28 butyrylcholinesterase Homo sapiens 83-97 34628225-3 2021 In this study, novel drug candidates were designed and synthesized by the covalent linkings of tacrine, a previously used anti-AD acetylcholinesterase (AChE) inhibitor, and dipicolylamine, an beta-amyloid (Abeta) aggregation inhibitor. tha 95-102 acetylcholinesterase Mus musculus 152-156 34628225-4 2021 Most tacrine-dipicolylamine dimers potently inhibited AChE and Abeta1-42 aggregation in vitro, and 13a exhibited nanomolar level inhibition. tha 5-12 acetylcholinesterase Mus musculus 54-58 34531295-0 2021 Tacrine induces endoplasmic reticulum-stressed apoptosis via disrupting the proper assembly of oligomeric acetylcholinesterase in cultured neuronal cells. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 34531295-4 2021 Here, we found tacrine could disrupt the proper trafficking of proline-rich membrane anchor-linked tetrameric AChE in the endoplasmic reticulum (ER). tha 15-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 110-114 34531295-5 2021 The exposure of tacrine in cells expressing AChE, e.g. neuron, caused an accumulation of the misfolded AChE in the ER. tha 16-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-48 34531295-5 2021 The exposure of tacrine in cells expressing AChE, e.g. neuron, caused an accumulation of the misfolded AChE in the ER. tha 16-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-107 34531295-9 2021 The ER stress and apoptosis, induced by tacrine, were proportional to the amount of AChE. tha 40-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 84-88 34531295-13 2021 Our study reports tacrine and other AChEIs disrupt the proper trafficking of AChE in the endoplasmic reticulum. tha 18-25 acetylcholinesterase (Cartwright blood group) Homo sapiens 77-81 34974209-7 2021 Representatively, the most potent compound against alpha-glycosidase enzyme, (S,S)-5b, was 12-times more potent than standard inhibitor acarbose; 7b and 8a as most potent compounds against cholinesterase enzymes, were around 5 and 13-times more potent than standard inhibitor tacrine against achethylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively. tha 276-283 butyrylcholinesterase Homo sapiens 349-353 35526766-4 2022 Being the first marketed drug for AD, tacrine reversibly inhibits AChE and thereby slows the breakdown of the chemical messenger acetylcholine (ACh) in the brain. tha 38-45 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 34443482-7 2021 In silico study suggested the compounds preferred the peripheral anionic site (PAS) to the catalytic anionic site (CAS), which was different from AChE inhibitors (tacrine and galanthamine). tha 163-170 acetylcholinesterase (Cartwright blood group) Homo sapiens 146-150 34471497-3 2021 Tacrine, a potent inhibitor of acetylcholinesterase (AChE) is the first FDA approved drug for the treatment of AD. tha 0-7 acetylcholinesterase Rattus norvegicus 31-51 34471497-3 2021 Tacrine, a potent inhibitor of acetylcholinesterase (AChE) is the first FDA approved drug for the treatment of AD. tha 0-7 acetylcholinesterase Rattus norvegicus 53-57 34273065-3 2022 In this work, focusing on the efficient cholinesterase inhibitory activity of tacrine, design and synthesis of novel arylisoxazole-tacrine analogues was developed. tha 78-85 butyrylcholinesterase Rattus norvegicus 40-54 34165688-5 2022 Tacrine was used as the reference drug and its IC50 values were 20.85 nM and 15.66 nM towards AChE and BuChE, respectively. tha 0-7 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 34120027-0 2021 1H-1,2,3-triazole grafted tacrine-chalcone conjugates as potential cholinesterase inhibitors with the evaluation of their behavioral tests and oxidative stress in mice brain cells. tha 26-33 butyrylcholinesterase Mus musculus 67-81 34120027-1 2021 The present paper explicates the synthesis of 1H-1,2,3-triazole tethered tacrine-chalcone conjugates and evaluation of their AChE and BuChE inhibitory activity. tha 73-80 acetylcholinesterase Mus musculus 125-129 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 52-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-135 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 52-59 acetylcholinesterase (Cartwright blood group) Homo sapiens 137-141 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 52-59 brain derived neurotrophic factor Homo sapiens 158-191 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 52-59 brain derived neurotrophic factor Homo sapiens 193-197 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 231-238 acetylcholinesterase (Cartwright blood group) Homo sapiens 115-135 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 231-238 brain derived neurotrophic factor Homo sapiens 158-191 34156230-3 2021 We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine derivative with acetylcholinesterase (AChE) inhibition and brain-derived neurotrophic factor (BDNF) activation activity, by linking tacrine and a fragment of huperzine A. tha 231-238 brain derived neurotrophic factor Homo sapiens 193-197 34385868-6 2021 Ki value of Tacrine (TAC), the reference compound, was 68.6 +- 3.8 nM towards AChE. tha 12-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 34385868-6 2021 Ki value of Tacrine (TAC), the reference compound, was 68.6 +- 3.8 nM towards AChE. tha 21-24 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 35526766-5 2022 However, the atomic level of interactions of tacrine towards human AChE (hAChE) is unknown for years. tha 45-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 67-71 35526766-5 2022 However, the atomic level of interactions of tacrine towards human AChE (hAChE) is unknown for years. tha 45-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-78 35526766-6 2022 Hence, in the current study, we report the X-ray structure of hAChE-tacrine complex at 2.85 A resolution. tha 68-75 acetylcholinesterase (Cartwright blood group) Homo sapiens 62-67 35526766-7 2022 The conformational heterogeneity of tacrine within the electron density was addressed with the help of molecular mechanics assisted methods and the low-energy ligand configuration is reported, which provides a mechanistic explanation for the high binding affinity of tacrine towards AChE. tha 36-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 283-287 35526766-7 2022 The conformational heterogeneity of tacrine within the electron density was addressed with the help of molecular mechanics assisted methods and the low-energy ligand configuration is reported, which provides a mechanistic explanation for the high binding affinity of tacrine towards AChE. tha 267-274 acetylcholinesterase (Cartwright blood group) Homo sapiens 283-287 35225413-6 2022 It should be noted that most of the synthesized compounds were more potent than standard inhibitor tacrine (TAC) against AChE. tha 99-106 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 35132681-2 2022 The obtained results showed that most of the synthesized compounds exhibited high to good anti-AChE and anti-BChE activity in the range of nanomolar concentrations in comparison to tacrine as a positive control. tha 181-188 butyrylcholinesterase Homo sapiens 109-113 35623141-0 2022 Discovery of novel tacrine derivatives as potent antiproliferative agents with CDKs inhibitory property. tha 19-26 cyclin dependent kinase 2 Homo sapiens 79-83 35225413-6 2022 It should be noted that most of the synthesized compounds were more potent than standard inhibitor tacrine (TAC) against AChE. tha 108-111 acetylcholinesterase (Cartwright blood group) Homo sapiens 121-125 35279105-1 2022 PURPOSE: To find the best short-term daily recombinant human erythropoietin (rhEPO)-based treatment protocols for blood-saving purpose in THA. tha 138-141 erythropoietin Homo sapiens 61-75 35098414-5 2022 Accumulated evidence reveals that Kv channels, which are broadly expressed in brain and possess crucial functions in modulating the neuronal activity, are inhibited by several acetylcholinesterase (AChE) inhibitors, such as tacrine, bis(7)-tacrine, donepezil and galantamine. tha 224-231 acetylcholinesterase (Cartwright blood group) Homo sapiens 176-196 35098414-5 2022 Accumulated evidence reveals that Kv channels, which are broadly expressed in brain and possess crucial functions in modulating the neuronal activity, are inhibited by several acetylcholinesterase (AChE) inhibitors, such as tacrine, bis(7)-tacrine, donepezil and galantamine. tha 224-231 acetylcholinesterase (Cartwright blood group) Homo sapiens 198-202