PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 8416935-6 1993 However, 1-methyl-4-phenylpyridinium and tetrabenazine, the other principal inhibitor of vesicular amine transport, compete very poorly with reserpine for binding, suggesting that they interact with CGAT at distinct sites. Tetrabenazine 41-54 solute carrier family 18 member A1 Rattus norvegicus 199-203 7912402-4 1994 COS cell hSVMT expression yielded nanomolar affinities for tetrabenazine and reserpine, micromolar affinities for haloperidol, GBR12909, serotonin, mazindol, nomifensin and d-amphetamine, while dopamine, epinephrine, norepinephrine and histamine each displayed millimolar affinities. Tetrabenazine 59-72 solute carrier family 18 member A2 Homo sapiens 9-14 8489249-3 1993 Tetrabenazine (TBZ)-displaceable [3H]ketanserin binding was used to label the granular 5-HT transporter. Tetrabenazine 0-13 solute carrier family 6 member 4 Homo sapiens 87-103 8489249-3 1993 Tetrabenazine (TBZ)-displaceable [3H]ketanserin binding was used to label the granular 5-HT transporter. Tetrabenazine 15-18 solute carrier family 6 member 4 Homo sapiens 87-103 8313393-2 1993 In psychopharmacologic investigations, the compound shows the properties expected of an MAO inhibitor, antagonizing the effects of reserpine, tetrabenazine, and 5-hydroxytryptophan in rats and mice, and suppressing rapid eye movement sleep in cats. Tetrabenazine 142-155 monoamine oxidase A Rattus norvegicus 88-91 1993899-4 1991 Theophylline, tetrabenazine, and angiotensin II also increased the rate of proenkephalin synthesis (three- to eight-fold). Tetrabenazine 14-27 proenkephalin Bos taurus 75-88 8473893-8 1993 Additionally, tetrabenazine binding showed a consistent shoulder in the region of synaptophysin. Tetrabenazine 14-27 synaptophysin Bos taurus 82-95 1861155-6 1991 Addition of tetrabenazine, an inhibitor of catecholamine uptake into chromaffin vesicles, during radiolabeling and a 6-h chase period caused enhanced proenkephalin processing. Tetrabenazine 12-25 proenkephalin Bos taurus 150-163 1970506-7 1990 The tetrabenazine effect on TH and pEK mRNA was reduced by alpha-amanitin, suggesting transcriptionally-mediated regulation. Tetrabenazine 4-17 tyrosine hydroxylase Bos taurus 28-30 1970506-7 1990 The tetrabenazine effect on TH and pEK mRNA was reduced by alpha-amanitin, suggesting transcriptionally-mediated regulation. Tetrabenazine 4-17 proenkephalin Bos taurus 35-38 3264161-5 1988 Moreover, [3H]MPP+ uptake is blocked by the monoamine transporter inhibitors tetrabenazine and reserpine. Tetrabenazine 77-90 solute carrier family 18 member A2 Homo sapiens 44-65 35429504-6 2022 As expected, dopamine accumulation was increased with l-DOPA addition or VMAT2-overexpression, and dopamine synthesis decreased further with added dopamine, the VMAT2 inhibitor tetrabenazine or D2 auto-receptor activation with quinpirole, accordingly to the known synaptic effects of these treatments. Tetrabenazine 177-190 solute carrier family 18 member A2 Rattus norvegicus 161-166 34491372-1 2022 PURPOSE: Deutetrabenazine is a deuterated form of tetrabenazine with a confirmed lower rate of CYP2D6 metabolism of the active metabolites, alpha- and beta-HTBZ. Tetrabenazine 50-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 95-101 34282360-4 2021 Vesicular monoamine transporter2 (VMAT2) inhibitors (Tetrabenazine, Deutetrabenazine, and Valbenazine) are new agents introduced in the last decade for treating some of movement disorders, in particular tardive dyskinesia, Huntington chorea, and Tourette syndrome. Tetrabenazine 53-66 solute carrier family 18 member A2 Homo sapiens 0-32 34282360-4 2021 Vesicular monoamine transporter2 (VMAT2) inhibitors (Tetrabenazine, Deutetrabenazine, and Valbenazine) are new agents introduced in the last decade for treating some of movement disorders, in particular tardive dyskinesia, Huntington chorea, and Tourette syndrome. Tetrabenazine 53-66 solute carrier family 18 member A2 Homo sapiens 34-39 3346672-8 1988 Finally, dopamine and 5-hydroxytryptamine depleted from their striatal stores by tetrabenazine were able to displace SR 95191 from the active site of MAO-A. Tetrabenazine 81-94 monoamine oxidase A Rattus norvegicus 150-155 3380081-6 1988 Tetrabenazine, an inhibitor of the monoamine transporter of chromaffin granules, displaced [3H]ketanserin binding. Tetrabenazine 0-13 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 35-56 3380081-14 1988 It is concluded that nonspecific displaceable binding sites of [3H]ketanserin previously described in the striatum are tetrabenazine binding sites associated with the synaptic vesicle monoamine transporter. Tetrabenazine 119-132 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 184-205 3336349-0 1988 Hydrophobicity of the tetrabenazine-binding site of the chromaffin granule monoamine transporter. Tetrabenazine 22-35 solute carrier family 18 member A2 Homo sapiens 75-96 3336349-1 1988 The catecholamine uptake inhibitor tetrabenazine (TBZ) binds to a high affinity site on the chromaffin granule membrane, presumably on the monoamine transporter. Tetrabenazine 35-48 solute carrier family 18 member A2 Homo sapiens 139-160 3336349-1 1988 The catecholamine uptake inhibitor tetrabenazine (TBZ) binds to a high affinity site on the chromaffin granule membrane, presumably on the monoamine transporter. Tetrabenazine 50-53 solute carrier family 18 member A2 Homo sapiens 139-160 3900292-2 1985 Catecholamine-depleting drugs, such as tetrabenazine, and cyclic nucleotide-elevating drugs, including forskolin, 8-bromo-cyclic AMP, and theophylline, increase chromaffin cell enkephalin-containing peptide levels but fail to increase dopamine beta-hydroxylase. Tetrabenazine 39-52 dopamine beta-hydroxylase Homo sapiens 235-260 3951433-5 1986 Transport occurs through the monoamine transporter since it is blocked by the same inhibitors, tetrabenazine and reserpine, and also by the transporter substrates noradrenaline and serotonin. Tetrabenazine 95-108 solute carrier family 18 member A2 Bos taurus 29-50 3569299-1 1987 The monoamine transporter of chromaffin granule membrane has two distinct high-affinity binding sites for tetrabenazine and reserpine, which can be assayed by [3H]dihydrotetrabenazine and [3H]reserpine binding, respectively. Tetrabenazine 106-119 solute carrier family 18 member A2 Homo sapiens 4-25 6197309-4 1983 Using a different approach, it was found that dopamine and serotonin released from their stores in rat striatum by tetrabenazine could displace CGP 11305 A from the MAO A active site in vivo, in contrast to clorgyline. Tetrabenazine 115-128 monoamine oxidase A Rattus norvegicus 165-170 6183051-8 1982 Reserpine and tetrabenazine depleted 5-HT and partially depleted substance P and TRH in the ventral cord, but had no effect on either methionine-enkephalin or somatostatin. Tetrabenazine 14-27 thyrotropin releasing hormone Rattus norvegicus 81-84 6174352-2 1981 Reserpine and tetrabenazine, but not p-chlorophenylalanine caused a partial depletion of ventral spinal cord substance P (SP) and thyrotropin-releasing hormone (TRH). Tetrabenazine 14-27 tachykinin precursor 1 Homo sapiens 109-120 6174352-2 1981 Reserpine and tetrabenazine, but not p-chlorophenylalanine caused a partial depletion of ventral spinal cord substance P (SP) and thyrotropin-releasing hormone (TRH). Tetrabenazine 14-27 tachykinin precursor 1 Homo sapiens 122-124 6174352-2 1981 Reserpine and tetrabenazine, but not p-chlorophenylalanine caused a partial depletion of ventral spinal cord substance P (SP) and thyrotropin-releasing hormone (TRH). Tetrabenazine 14-27 thyrotropin releasing hormone Homo sapiens 130-159 6174352-4 1981 The rates of loss and recovery of SP and TRH after reserpine and tetrabenazine were different from that of 5-hydroxytryptamine (5-HT), though in the ventral spinal cord these two peptides probably coexist with 5-HT in the terminals of bulbospinal neurones. Tetrabenazine 65-78 tachykinin precursor 1 Homo sapiens 34-36 6794869-0 1981 [Binding of a tetrabenazine derivative to the monoamine transporter of the chromaffin granule membrane]. Tetrabenazine 14-27 solute carrier family 18 member A2 Homo sapiens 46-67 33038289-5 2021 Both studies confirmed longer half-lives for active metabolites and lower peak-to-trough fluctuations for the sum of the metabolites (total [alpha+beta]-HTBZ) following deutetrabenazine compared with tetrabenazine (3- to 4-fold and 11-fold, respectively) in steady-state conditions. Tetrabenazine 172-185 amyloid beta precursor protein Homo sapiens 141-151 32771528-10 2020 On the other hand, while tetrabenazine had mild effects on cFOS counts, it reduced functional connectivity across the entire brain, cortical node degree, and global efficiency. Tetrabenazine 25-38 FBJ osteosarcoma oncogene Mus musculus 59-63 32770257-4 2020 OBJECTIVES: Recent studies demonstrated that the atypical DA transport (DAT) inhibitor (S)-CE-123 reversed tetrabenazine-induced motivational deficits, increased progressive ratio (PROG) lever pressing, and increased extracellular DA in the nucleus accumbens. Tetrabenazine 107-120 solute carrier family 6 member 3 Homo sapiens 72-75 33174440-3 2021 Deutetrabenazine was adapted from an earlier VMAT2 inhibitor, tetrabenazine, by substituting three deuterium isotopes in place of three hydrogen isotopes at the site of metabolic degradation to improve upon the pharmacokinetics of the parent compound. Tetrabenazine 3-16 solute carrier family 18 member A2 Homo sapiens 45-50 33038289-6 2021 Deutetrabenazine doses estimated to provide total (alpha+beta)-HTBZ exposure comparable to tetrabenazine 25 mg were 11.4-13.2 mg. Food had no effect on exposure to total (alpha+beta)-HTBZ, as measured by AUC. Tetrabenazine 3-16 amyloid beta precursor protein Homo sapiens 51-61 33038289-7 2021 Although the total (alpha+beta)-HTBZ Cmax of deutetrabenazine was increased by 50% in the presence of food, it remained lower than that of tetrabenazine. Tetrabenazine 48-61 amyloid beta precursor protein Homo sapiens 20-30 30870235-1 2019 OBJECTIVES: The aim of this study was to review our "real-world" experience with the vesicular monoamine transporter 2 (VMAT2) inhibitors tetrabenazine (TBZ), deutetrabenazine (DTBZ), and valbenazine (VBZ) for treatment of hyperkinetic movement disorders. Tetrabenazine 138-151 solute carrier family 18 member A2 Homo sapiens 85-118 32454050-4 2020 Optimization of the pharmacology of tetrabenazine has since led to the approval of two new VMAT2 inhibitors, deutetrabenazine and valbenazine. Tetrabenazine 36-49 solute carrier family 18 member A2 Homo sapiens 91-96 32329312-4 2020 Results: Thirteen clinical cases, ten of which involved tetrabenazine, were identified in which VMAT2 inhibitors were prescribed in patients with current or past NMS episodes. Tetrabenazine 56-69 solute carrier family 18 member A2 Homo sapiens 96-101 31209099-10 2019 Hence, we hypothesize that TBZ facilitates exocytosis by increasing Ca2+ release through the endoplasmic reticulum ryanodine receptor channel (RyR). Tetrabenazine 27-30 ryanodine receptor 2 Rattus norvegicus 115-141 31209099-10 2019 Hence, we hypothesize that TBZ facilitates exocytosis by increasing Ca2+ release through the endoplasmic reticulum ryanodine receptor channel (RyR). Tetrabenazine 27-30 ryanodine receptor 2 Rattus norvegicus 143-146 29455579-4 2019 These agents were pharmacologically modified from tetrabenazine, a VMAT2 inhibitor used off-label in the treatment of tardive dyskinesia. Tetrabenazine 50-63 solute carrier family 18 member A2 Homo sapiens 67-72 30870235-1 2019 OBJECTIVES: The aim of this study was to review our "real-world" experience with the vesicular monoamine transporter 2 (VMAT2) inhibitors tetrabenazine (TBZ), deutetrabenazine (DTBZ), and valbenazine (VBZ) for treatment of hyperkinetic movement disorders. Tetrabenazine 138-151 solute carrier family 18 member A2 Homo sapiens 120-125 30870235-1 2019 OBJECTIVES: The aim of this study was to review our "real-world" experience with the vesicular monoamine transporter 2 (VMAT2) inhibitors tetrabenazine (TBZ), deutetrabenazine (DTBZ), and valbenazine (VBZ) for treatment of hyperkinetic movement disorders. Tetrabenazine 153-156 solute carrier family 18 member A2 Homo sapiens 85-118 30198706-3 2019 The development of in vivo imaging radiotracers for VMAT2 is a story of starting with a well-characterized clinically used drug (tetrabenazine) which had a pharmacologically active metabolite: that metabolite that was in stepwise fashion refined and modified to provide both carbon-11 and fluorine-18 labeled VMAT2 radiotracers that are now used for human PET studies of neurodegenerative and psychiatric diseases. Tetrabenazine 129-142 solute carrier family 18 member A2 Homo sapiens 52-57 30198706-3 2019 The development of in vivo imaging radiotracers for VMAT2 is a story of starting with a well-characterized clinically used drug (tetrabenazine) which had a pharmacologically active metabolite: that metabolite that was in stepwise fashion refined and modified to provide both carbon-11 and fluorine-18 labeled VMAT2 radiotracers that are now used for human PET studies of neurodegenerative and psychiatric diseases. Tetrabenazine 129-142 solute carrier family 18 member A2 Homo sapiens 309-314 29996061-4 2018 Areas covered: Deutetrabenazine is the first deuterated drug and second drug after tetrabenazine, the classic vesicular monoamine transporter type 2 (VMAT2) inhibitor, to receive approval for the treatment of chorea associated with HD. Tetrabenazine 18-31 solute carrier family 18 member A2 Homo sapiens 110-148 30306450-3 2018 At present, there are three commercially available VMAT2 inhibitors: tetrabenazine, deutetrabenazine, and valbenazine. Tetrabenazine 69-82 solute carrier family 18 member A2 Homo sapiens 51-56 29408363-4 2018 In the present work, we evaluated the effect of caffeine on anergia induced by the VMAT-2 inhibitor tetrabenazine (TBZ), which depletes DA. Tetrabenazine 100-113 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 83-89 29408363-4 2018 In the present work, we evaluated the effect of caffeine on anergia induced by the VMAT-2 inhibitor tetrabenazine (TBZ), which depletes DA. Tetrabenazine 115-118 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 83-89 29433808-5 2018 Characterization of the VMAT2 inhibitor tetrabenazine, which was identified as a therapeutic agent for TD in older clinical trials, has yielded two distinct pharmacologic strategies to optimize response. Tetrabenazine 40-53 solute carrier family 18 member A2 Homo sapiens 24-29 29996061-4 2018 Areas covered: Deutetrabenazine is the first deuterated drug and second drug after tetrabenazine, the classic vesicular monoamine transporter type 2 (VMAT2) inhibitor, to receive approval for the treatment of chorea associated with HD. Tetrabenazine 18-31 solute carrier family 18 member A2 Homo sapiens 150-155 29309800-0 2018 Partial reversal of the effort-related motivational effects of tetrabenazine with the MAO-B inhibitor deprenyl (selegiline): Implications for treating motivational dysfunctions. Tetrabenazine 63-76 monoamine oxidase B Homo sapiens 86-91 29484607-5 2018 The vesicular monoamine transporter 2 (VMAT2) inhibitors, which include tetrabenazine, deutetrabenazine, and valbenazine, are considered the treatment of choice for most patients with TD. Tetrabenazine 72-85 solute carrier family 18 member A2 Homo sapiens 4-37 29484607-5 2018 The vesicular monoamine transporter 2 (VMAT2) inhibitors, which include tetrabenazine, deutetrabenazine, and valbenazine, are considered the treatment of choice for most patients with TD. Tetrabenazine 72-85 solute carrier family 18 member A2 Homo sapiens 39-44 29484607-6 2018 Deutetrabenazine-a deuterated version of tetrabenazine-and valbenazine, the purified parent product of one of the main tetrabenazine metabolites, are novel VMAT2 inhibitors and the only drugs to receive approval from the US FDA for the treatment of TD. Tetrabenazine 3-16 solute carrier family 18 member A2 Homo sapiens 156-161 29484607-6 2018 Deutetrabenazine-a deuterated version of tetrabenazine-and valbenazine, the purified parent product of one of the main tetrabenazine metabolites, are novel VMAT2 inhibitors and the only drugs to receive approval from the US FDA for the treatment of TD. Tetrabenazine 41-54 solute carrier family 18 member A2 Homo sapiens 156-161 29309800-7 2018 These effects of 0.75mg/kg tetrabenazine were attenuated by co-administration of the MAO-B inhibitor deprenyl (selegiline). Tetrabenazine 27-40 monoamine oxidase B Homo sapiens 85-90 27819145-4 2016 Areas covered: Since the approval of tetrabenazine, the classic VMAT2 inhibitor, in the treatment of chorea associated with Huntington disease (HD), other VMAT2 inhibitors (e.g. deutetrabenazine and valbenazine) have been studied in the treatment of HD-related chorea, tardive dyskinesia and tics associated with Tourette syndrome. Tetrabenazine 37-50 solute carrier family 18 member A2 Homo sapiens 64-69 29497277-3 2018 Deutetrabenazine is a deuterated form of tetrabenazine and is a vesicular monoamine transporter 2 (VMAT2) inhibitor. Tetrabenazine 3-16 solute carrier family 18 member A2 Homo sapiens 64-97 29497277-3 2018 Deutetrabenazine is a deuterated form of tetrabenazine and is a vesicular monoamine transporter 2 (VMAT2) inhibitor. Tetrabenazine 3-16 solute carrier family 18 member A2 Homo sapiens 99-104 29120264-5 2018 Expert commentary: Inhibitors of presynaptic vesicular monoamine transporter type 2 (VMAT2) that cause striatal dopamine depletion, such as tetrabenazine, deutetrabenazine, and valbenazine, are considered the treatment of choice in patients with chorea. Tetrabenazine 140-153 solute carrier family 18 member A2 Homo sapiens 45-83 29120264-5 2018 Expert commentary: Inhibitors of presynaptic vesicular monoamine transporter type 2 (VMAT2) that cause striatal dopamine depletion, such as tetrabenazine, deutetrabenazine, and valbenazine, are considered the treatment of choice in patients with chorea. Tetrabenazine 140-153 solute carrier family 18 member A2 Homo sapiens 85-90 28776237-10 2017 CONCLUSIONS: Based on relative abundance and potency, [+]-beta-HTBZ appears to be the primary contributor to VMAT2 inhibition by TBZ, a finding in contrast with the generally held assertion that [+]-alpha-HTBZ is the major contributor. Tetrabenazine 64-67 solute carrier family 18 member A2 Homo sapiens 109-114 28776237-11 2017 [-]-alpha-HTBZ, the other abundant TBZ metabolite, has much lower VMAT2 inhibitory potency than [+]-beta-HTBZ, but increased affinity for other CNS targets, which may contribute to off-target effects of TBZ. Tetrabenazine 11-14 solute carrier family 18 member A2 Homo sapiens 66-71 28404690-4 2017 Radioligand-binding studies were conducted to assess and compare valbenazine, tetrabenazine, and their respective metabolites in their abilities to selectively and potently inhibit [3H]-HTBZ binding to VMAT2 in rat striatal, rat forebrain, and human platelet homogenates. Tetrabenazine 78-91 solute carrier family 18 member A2 Rattus norvegicus 202-207 28404690-9 2017 In vivo studies measuring ptosis and prolactin secretion in the rat confirmed the specific and dose-dependent interactions of tetrabenazine and R,R,R-HTBZ with VMAT2. Tetrabenazine 126-139 solute carrier family 18 member A2 Rattus norvegicus 160-165 29080203-1 2017 Oral deutetrabenazine (Austedo ), a reversible inhibitor of vesicular monoamine transporter type 2 (VMAT2) that is structurally related to tetrabenazine is approved for the treatment of chorea symptoms associated with Huntington"s disease (HD). Tetrabenazine 8-21 solute carrier family 18 member A2 Homo sapiens 60-98 29080203-1 2017 Oral deutetrabenazine (Austedo ), a reversible inhibitor of vesicular monoamine transporter type 2 (VMAT2) that is structurally related to tetrabenazine is approved for the treatment of chorea symptoms associated with Huntington"s disease (HD). Tetrabenazine 8-21 solute carrier family 18 member A2 Homo sapiens 100-105 28905625-0 2017 Oral Ingestion and Intraventricular Injection of Curcumin Attenuates the Effort-Related Effects of the VMAT-2 Inhibitor Tetrabenazine: Implications for Motivational Symptoms of Depression. Tetrabenazine 120-133 solute carrier family 18 member A2 Homo sapiens 103-109 28742396-5 2017 Valbenazine is a modified metabolite of the vesicular monoamine transporter 2 (VMAT-2) inhibitor tetrabenazine, which is approved for the treatment of the hyperkinetic movement disorder, Huntington"s disease. Tetrabenazine 97-110 solute carrier family 18 member A2 Homo sapiens 44-77 28742396-5 2017 Valbenazine is a modified metabolite of the vesicular monoamine transporter 2 (VMAT-2) inhibitor tetrabenazine, which is approved for the treatment of the hyperkinetic movement disorder, Huntington"s disease. Tetrabenazine 97-110 solute carrier family 18 member A2 Homo sapiens 79-85 27570189-16 2016 A similar differential secretory dysfunction is observed in CB cells treated with tetrabenazine, a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2). Tetrabenazine 82-95 solute carrier family 18 member A2 Rattus norvegicus 126-159 27570189-16 2016 A similar differential secretory dysfunction is observed in CB cells treated with tetrabenazine, a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2). Tetrabenazine 82-95 solute carrier family 18 member A2 Rattus norvegicus 161-166 27819145-6 2016 Expert commentary: Because of differences in pharmacology and pharmacokinetics these new VMAT2 inhibitors promise to be at least as effective as tetrabenazine but with a lower risk of adverse effects, such as sedation, insomnia, depression, parkinsonism, and akathisia. Tetrabenazine 145-158 solute carrier family 18 member A2 Homo sapiens 89-94 27821772-7 2016 These experiments provide significant insight into the role of proton translocation in the conformational dynamics of a mammalian H+-coupled antiporter, and also identify key aspects of the mode of action and binding of two potent inhibitors of VMAT2: reserpine binds the cytoplasm-facing conformation, and tetrabenazine binds the lumen-facing conformation. Tetrabenazine 307-320 solute carrier family 18 member A2 Homo sapiens 245-250 27381871-9 2016 DiHTBZ enantiomers were catalyzed mainly by CYP2C19 and the predicted clearance suggests that liver metabolism is the main route for TBZ elimination which supports the literature data. Tetrabenazine 3-6 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 44-51 26590367-0 2016 The MAO-B inhibitor deprenyl reduces the oral tremor and the dopamine depletion induced by the VMAT-2 inhibitor tetrabenazine. Tetrabenazine 112-125 monoamine oxidase B Homo sapiens 4-9 26590367-0 2016 The MAO-B inhibitor deprenyl reduces the oral tremor and the dopamine depletion induced by the VMAT-2 inhibitor tetrabenazine. Tetrabenazine 112-125 solute carrier family 18 member A2 Homo sapiens 95-101 26590367-2 2016 Via inhibition of the vesicular monoamine transporter (VMAT-2), TBZ blocks dopamine (DA) storage and depletes striatal DA; this drug also has been shown to induce Parkinsonian motor side effects in patients. Tetrabenazine 64-67 solute carrier family 18 member A2 Homo sapiens 55-61 26105139-4 2016 In the present studies the effort-related effects of the vesicular monoamine transport (VMAT-2) inhibitor tetrabenazine (TBZ) were investigated. Tetrabenazine 106-119 solute carrier family 18 member A2 Homo sapiens 88-94 26105139-4 2016 In the present studies the effort-related effects of the vesicular monoamine transport (VMAT-2) inhibitor tetrabenazine (TBZ) were investigated. Tetrabenazine 121-124 solute carrier family 18 member A2 Homo sapiens 88-94 24905523-6 2014 Tetrabenazine-treatment (1mg/kg sc) depletes the transmitters from their stores in the nerve terminals of the catecholaminergic neurons and blocks the acquisition of a CAR. Tetrabenazine 0-13 nuclear receptor subfamily 1, group I, member 3 Rattus norvegicus 168-171 25323625-0 2015 The VMAT-2 inhibitor tetrabenazine alters effort-related decision making as measured by the T-maze barrier choice task: reversal with the adenosine A2A antagonist MSX-3 and the catecholamine uptake blocker bupropion. Tetrabenazine 21-34 solute carrier family 18 member A2 Homo sapiens 4-10 25323625-2 2015 Animal tests can model these motivational symptoms, and the present studies characterized the effort-related effects of the vesicular monoamine transport (VMAT-2) inhibitor tetrabenazine. Tetrabenazine 173-186 solute carrier family 18 member A2 Homo sapiens 155-161 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 138-151 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 159-192 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 138-151 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 194-199 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 138-151 pancreatic and duodenal homeobox 1 Mus musculus 258-262 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 138-151 neurogenin 3 Mus musculus 305-309 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 153-156 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 159-192 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 153-156 pancreatic and duodenal homeobox 1 Mus musculus 258-262 25762295-1 2016 Pluripotent stem cells are considered as a cell source for replacement therapies for pancreatic beta cells and other organs.We identified tetrabenazine (TBZ), vesicular monoamine transporter 2 (VMAT2) inhibitor as a promoter of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Ngn3-positive endocrine progenitor cells. Tetrabenazine 153-156 neurogenin 3 Mus musculus 305-309 25858023-5 2015 METHODS: The effects of ketamine and other NMDAR antagonists to reverse tetrabenazine-induced ptosis were examined and compared with their antidepressant-like effects in the tail suspension test (TST) in mice. Tetrabenazine 72-85 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 43-48 25858023-6 2015 RESULTS: All the NMDAR antagonists tested produced a partial reversal of tetrabenazine-induced ptosis and, as expected, reduced immobility in the TST. Tetrabenazine 73-86 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 17-22 25858023-8 2015 CONCLUSION: The ability to reverse tetrabenazine-induced ptosis is a class effect of NMDAR antagonists. Tetrabenazine 35-48 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 85-90 25759301-1 2015 The cardinal motor symptoms of Parkinson"s disease (PD) include resting tremor, akinesia, bradykinesia, and rigidity, and these motor abnormalities can be modeled in rodents by administration of the VMAT-2 (type-2 vesicular monoamine transporter) inhibitor tetrabenazine (9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7, 11b hexahydrobenzo[a]quinolizin-2-one; TBZ). Tetrabenazine 257-270 solute carrier family 18 member A2 Rattus norvegicus 199-205 25467156-1 2014 Dihydrotetrabenazine (DTBZ) derivatized from (+) Tetrabenazine (TBZ) has been used for imaging the expression of VMAT2 when labeled with (11)C (t1/2=20.3 min) or (18)F (t1/2=110 min) in neurodegenerative diseases or pancreatic beta-cell. Tetrabenazine 45-62 solute carrier family 18 member A2 Rattus norvegicus 113-118 25467156-1 2014 Dihydrotetrabenazine (DTBZ) derivatized from (+) Tetrabenazine (TBZ) has been used for imaging the expression of VMAT2 when labeled with (11)C (t1/2=20.3 min) or (18)F (t1/2=110 min) in neurodegenerative diseases or pancreatic beta-cell. Tetrabenazine 23-26 solute carrier family 18 member A2 Rattus norvegicus 113-118 24937131-0 2014 The VMAT-2 inhibitor tetrabenazine affects effort-related decision making in a progressive ratio/chow feeding choice task: reversal with antidepressant drugs. Tetrabenazine 21-34 solute carrier family 18 member A2 Homo sapiens 4-10 24937131-3 2014 Tasks measuring effort-based decision making can be used as animal models of the motivational symptoms of depression, and the present studies characterized the effort-related effects of the vesicular monoamine transport (VMAT-2) inhibitor tetrabenazine. Tetrabenazine 239-252 solute carrier family 18 member A2 Homo sapiens 221-227 24937131-9 2014 The adenosine A2A antagonist MSX-3, the antidepressant and catecholamine uptake inhibitor bupropion, and the MAO-B inhibitor deprenyl, all reversed the impairments induced by tetrabenazine. Tetrabenazine 175-188 monoamine oxidase B Homo sapiens 109-114 24018103-4 2013 VMAT2 is also a target of tetrabenazine, a drug used in the treatment of hyperkinetic movement disorders, including TD. Tetrabenazine 26-39 solute carrier family 18 member A2 Homo sapiens 0-5 24002822-9 2014 Depletion of cellular histamine with tetrabenazine, an inhibitor of vesicular monoamine transporter-2, did not affect granule maturation. Tetrabenazine 37-50 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 68-101 24305809-9 2013 A behaviorally active dose of tetrabenazine decreased extracellular DA in nucleus accumbens and increased expression of DARPP-32 in accumbens medium spiny neurons in a pattern indicative of reduced transmission at both D1 and D2 DA receptors. Tetrabenazine 30-43 protein phosphatase 1 regulatory inhibitor subunit 1B Homo sapiens 120-128 24062308-3 2013 Tetrabenazine (TBZ) is a non-competitive inhibitor of VMAT2 that is used in the treatment of hyperkinetic disorders associated with Huntington disease and Tourette syndrome. Tetrabenazine 0-13 solute carrier family 18 member A2 Homo sapiens 54-59 24062308-3 2013 Tetrabenazine (TBZ) is a non-competitive inhibitor of VMAT2 that is used in the treatment of hyperkinetic disorders associated with Huntington disease and Tourette syndrome. Tetrabenazine 15-18 solute carrier family 18 member A2 Homo sapiens 54-59 24062308-5 2013 However, the precise mechanism of TBZ interaction with VMAT2 remains unknown. Tetrabenazine 34-37 solute carrier family 18 member A2 Homo sapiens 55-60 24062308-10 2013 Our results provide a novel insight into the mechanism of transport and TBZ binding by VMAT2. Tetrabenazine 72-75 solute carrier family 18 member A2 Homo sapiens 87-92 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 43-56 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 69-102 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 43-56 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 104-109 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 43-56 pancreatic and duodenal homeobox 1 Mus musculus 169-173 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 43-56 neurogenin 3 Mus musculus 216-223 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 43-56 neurogenin 3 Mus musculus 251-255 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 58-61 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 69-102 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 58-61 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 104-109 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 58-61 pancreatic and duodenal homeobox 1 Mus musculus 169-173 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 58-61 neurogenin 3 Mus musculus 216-223 24316738-3 2014 The present study identified reserpine and tetrabenazine (TBZ), both vesicular monoamine transporter 2 (VMAT2) inhibitors, as promoters of late-stage differentiation of Pdx1-positive pancreatic progenitor cells into Neurog3 (referred to henceforth as Ngn3)-positive endocrine precursors. Tetrabenazine 58-61 neurogenin 3 Mus musculus 251-255 24305809-0 2013 Effort-related motivational effects of the VMAT-2 inhibitor tetrabenazine: implications for animal models of the motivational symptoms of depression. Tetrabenazine 60-73 solute carrier family 18 member A2 Homo sapiens 43-49 24305809-4 2013 Tetrabenazine produces depressive symptoms in humans and, because of its selective inhibition of VMAT-2, it preferentially depletes dopamine (DA). Tetrabenazine 0-13 solute carrier family 18 member A2 Homo sapiens 97-103 23280482-0 2013 Analysis of CYP2D6 genotype and response to tetrabenazine. Tetrabenazine 44-57 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 12-18 24255799-1 2013 BACKGROUND: Although tetrabenazine, a drug that depletes presynaptic dopamine by inhibiting vesicular monoamine transporter 2 (VMAT2), was approved by the U.S. Food and Drug Administration in 2008 for the treatment of chorea associated with Huntington"s disease (HD), there is a paucity of data on its long-term efficacy and safety. Tetrabenazine 21-34 solute carrier family 18 member A2 Homo sapiens 92-125 24255799-1 2013 BACKGROUND: Although tetrabenazine, a drug that depletes presynaptic dopamine by inhibiting vesicular monoamine transporter 2 (VMAT2), was approved by the U.S. Food and Drug Administration in 2008 for the treatment of chorea associated with Huntington"s disease (HD), there is a paucity of data on its long-term efficacy and safety. Tetrabenazine 21-34 solute carrier family 18 member A2 Homo sapiens 127-132 23867769-0 2013 The vesicular monoamine transporter (VMAT-2) inhibitor tetrabenazine induces tremulous jaw movements in rodents: implications for pharmacological models of parkinsonian tremor. Tetrabenazine 55-68 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 37-43 23867769-5 2013 The adenosine A2A antagonist MSX-3 (1.25-10.0mg/kg) significantly attenuated the TJMs induced by 2.0mg/kg TBZ in rats, and also significantly reduced the display of catalepsy and locomotor suppression induced by TBZ. Tetrabenazine 106-109 msh homeobox 3 Mus musculus 29-34 23867769-5 2013 The adenosine A2A antagonist MSX-3 (1.25-10.0mg/kg) significantly attenuated the TJMs induced by 2.0mg/kg TBZ in rats, and also significantly reduced the display of catalepsy and locomotor suppression induced by TBZ. Tetrabenazine 212-215 msh homeobox 3 Mus musculus 29-34 23867769-7 2013 MSX-3 (2.5-10.0mg/kg) also significantly reduced TBZ-induced TJMs in CD1 mice. Tetrabenazine 49-52 msh homeobox 3 Mus musculus 0-5 23867769-7 2013 MSX-3 (2.5-10.0mg/kg) also significantly reduced TBZ-induced TJMs in CD1 mice. Tetrabenazine 49-52 CD1 antigen complex Mus musculus 69-72 23867769-9 2013 TBZ (2.0mg/kg) significantly increased the number of c-Fos-positive cells in the VLS, which is indicative of reduced DA D2 receptor transmission, and 10.0mg/kg MSX-3 significantly attenuated the TBZ-induced c-Fos expression. Tetrabenazine 0-3 FBJ osteosarcoma oncogene Mus musculus 53-58 23867769-9 2013 TBZ (2.0mg/kg) significantly increased the number of c-Fos-positive cells in the VLS, which is indicative of reduced DA D2 receptor transmission, and 10.0mg/kg MSX-3 significantly attenuated the TBZ-induced c-Fos expression. Tetrabenazine 0-3 dopamine receptor D2 Mus musculus 120-131 23867769-9 2013 TBZ (2.0mg/kg) significantly increased the number of c-Fos-positive cells in the VLS, which is indicative of reduced DA D2 receptor transmission, and 10.0mg/kg MSX-3 significantly attenuated the TBZ-induced c-Fos expression. Tetrabenazine 0-3 FBJ osteosarcoma oncogene Mus musculus 207-212 23867769-9 2013 TBZ (2.0mg/kg) significantly increased the number of c-Fos-positive cells in the VLS, which is indicative of reduced DA D2 receptor transmission, and 10.0mg/kg MSX-3 significantly attenuated the TBZ-induced c-Fos expression. Tetrabenazine 195-198 msh homeobox 3 Mus musculus 160-165 23875622-8 2013 These results support a hypothetical model of GZ-793A interaction at more than one site on the VMAT2 protein, which explains its potent inhibition of dopamine uptake, dopamine release via a High-affinity tetrabenazine- and reserpine-sensitive site, dopamine release via a Low-affinity tetrabenazine- and reserpine-insensitive site, and a low-affinity interaction with the dihydrotetrabenazine binding site on VMAT2. Tetrabenazine 204-217 solute carrier family 18 member A2 Rattus norvegicus 95-100 23875622-8 2013 These results support a hypothetical model of GZ-793A interaction at more than one site on the VMAT2 protein, which explains its potent inhibition of dopamine uptake, dopamine release via a High-affinity tetrabenazine- and reserpine-sensitive site, dopamine release via a Low-affinity tetrabenazine- and reserpine-insensitive site, and a low-affinity interaction with the dihydrotetrabenazine binding site on VMAT2. Tetrabenazine 285-298 solute carrier family 18 member A2 Rattus norvegicus 95-100 23404442-3 2013 Radiolabelled analogues of tetrabenazine (TBZ; a low-molecular-weight, cell-permeant VMAT2-selective ligand) have been employed for pancreatic islet imaging in humans. Tetrabenazine 27-40 solute carrier family 18 member A2 Homo sapiens 85-90 23404442-3 2013 Radiolabelled analogues of tetrabenazine (TBZ; a low-molecular-weight, cell-permeant VMAT2-selective ligand) have been employed for pancreatic islet imaging in humans. Tetrabenazine 42-45 solute carrier family 18 member A2 Homo sapiens 85-90 23280482-2 2013 Following oral administration, tetrabenazine is hepatically transformed into 2 active metabolites that are CYP2D6 substrates. Tetrabenazine 31-44 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 107-113 23280482-4 2013 CYP2D6 genotyping was performed on sequential subjects treated with tetrabenazine, but results were not known at the time of titration. Tetrabenazine 68-81 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 22749259-7 2012 RESULTS: TBZ variably undergoes extensive first-pass metabolism to active metabolites, some of which are metabolized by the cytochrome P450 2D6 isozyme. Tetrabenazine 9-12 cytochrome P450 2D6 Homo sapiens 124-143 22698664-11 2012 Furthermore, the VMAT2-specific inhibitor tetrabenazine (TBZ) blocks uptake into the mCherry-positive compartment. Tetrabenazine 42-55 solute carrier family 18 member A2 Homo sapiens 17-22 22698664-11 2012 Furthermore, the VMAT2-specific inhibitor tetrabenazine (TBZ) blocks uptake into the mCherry-positive compartment. Tetrabenazine 57-60 solute carrier family 18 member A2 Homo sapiens 17-22 22296263-10 2012 To further unmask the mechanics governing extracellular dopamine levels we used intravenous injection of the vesicular monoamine transporter (VMAT2) inhibitor, tetrabenazine, to deplete dopamine storage and increase cytoplasmic dopamine in the nerve terminals. Tetrabenazine 160-173 solute carrier family 18 member A2 Rattus norvegicus 142-147 22296263-11 2012 Tetrabenazine almost abolished phasic dopamine release but increased extracellular dopamine to ~500 nM, presumably by inducing reverse transport by dopamine transporter (DAT). Tetrabenazine 0-13 solute carrier family 6 member 3 Rattus norvegicus 148-168 22296263-11 2012 Tetrabenazine almost abolished phasic dopamine release but increased extracellular dopamine to ~500 nM, presumably by inducing reverse transport by dopamine transporter (DAT). Tetrabenazine 0-13 solute carrier family 6 member 3 Rattus norvegicus 170-173 21669212-7 2011 Results show that TBZ was 11-fold more potent inhibiting DAT than SERT, and 2.5-fold more potent inhibiting VMAT2 than DAT. Tetrabenazine 18-21 solute carrier family 18 member A2 Rattus norvegicus 108-113 22198452-2 2012 This study examined augmenting response in treatment-resistant schizophrenia through the addition of tetrabenazine (TBZ), a presynaptic vesicular monoamine transporter (VMAT2) inhibitor. Tetrabenazine 101-114 solute carrier family 18 member A2 Homo sapiens 169-174 22198452-2 2012 This study examined augmenting response in treatment-resistant schizophrenia through the addition of tetrabenazine (TBZ), a presynaptic vesicular monoamine transporter (VMAT2) inhibitor. Tetrabenazine 116-119 solute carrier family 18 member A2 Homo sapiens 169-174 21982574-0 2011 Sigma receptor binding of tetrabenazine series tracers targeting VMAT2 in rat pancreas. Tetrabenazine 26-39 solute carrier family 18 member A2 Rattus norvegicus 65-70 21669212-1 2011 Tetrabenazine (TBZ), a benzoquinolizine derivative, binds with high affinity to the vesicular monoamine transporter-2 (VMAT2), inhibiting uptake of cytosolic monoamines. Tetrabenazine 0-13 solute carrier family 18 member A2 Rattus norvegicus 84-117 21669212-7 2011 Results show that TBZ was 11-fold more potent inhibiting DAT than SERT, and 2.5-fold more potent inhibiting VMAT2 than DAT. Tetrabenazine 18-21 solute carrier family 6 member 3 Rattus norvegicus 119-122 21669212-1 2011 Tetrabenazine (TBZ), a benzoquinolizine derivative, binds with high affinity to the vesicular monoamine transporter-2 (VMAT2), inhibiting uptake of cytosolic monoamines. Tetrabenazine 0-13 solute carrier family 18 member A2 Rattus norvegicus 119-124 20135628-6 2011 The classical VMAT2 inhibitor, tetrabenazine, has long been used for the treatment of chorea associated with Huntington"s disease in the United Kingdom, Canada, and Australia, and recently approved in the United States. Tetrabenazine 31-44 solute carrier family 18 member A2 Homo sapiens 14-19 21669212-1 2011 Tetrabenazine (TBZ), a benzoquinolizine derivative, binds with high affinity to the vesicular monoamine transporter-2 (VMAT2), inhibiting uptake of cytosolic monoamines. Tetrabenazine 15-18 solute carrier family 18 member A2 Rattus norvegicus 84-117 21669212-1 2011 Tetrabenazine (TBZ), a benzoquinolizine derivative, binds with high affinity to the vesicular monoamine transporter-2 (VMAT2), inhibiting uptake of cytosolic monoamines. Tetrabenazine 15-18 solute carrier family 18 member A2 Rattus norvegicus 119-124 21669212-7 2011 Results show that TBZ was 11-fold more potent inhibiting DAT than SERT, and 2.5-fold more potent inhibiting VMAT2 than DAT. Tetrabenazine 18-21 solute carrier family 6 member 3 Rattus norvegicus 57-60 21669212-7 2011 Results show that TBZ was 11-fold more potent inhibiting DAT than SERT, and 2.5-fold more potent inhibiting VMAT2 than DAT. Tetrabenazine 18-21 solute carrier family 6 member 4 Rattus norvegicus 66-70 21273402-6 2011 D1 receptor modulation of sEPSCs was absent in D1-YAC128 cells at the early symptomatic stage but was restored by treating the slices with tetrabenazine. Tetrabenazine 139-152 dopamine receptor D1 Mus musculus 0-11 21396745-0 2011 Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors. Tetrabenazine 30-43 solute carrier family 18 member A2 Homo sapiens 111-116 21396745-1 2011 Tetrabenazine (TBZ) ((+-)-1) and dihydrotetrabenazines (DHTBZ) are potent inhibitors of VMAT2. Tetrabenazine 0-13 solute carrier family 18 member A2 Homo sapiens 88-93 21396745-1 2011 Tetrabenazine (TBZ) ((+-)-1) and dihydrotetrabenazines (DHTBZ) are potent inhibitors of VMAT2. Tetrabenazine 15-18 solute carrier family 18 member A2 Homo sapiens 88-93 20869622-13 2010 TBZ is subject to important drug-drug interactions with inhibitors and inducers of cytochrome P450 (CYP) 2D6, reserpine, and lithium. Tetrabenazine 0-3 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 83-108 20420689-4 2010 A specific inhibitor of vesicular monoamine transporter (VMAT2) tetrabenazine (TBZ) has been recently approved by Food and Drug Administration for treatment of HD patients in the USA. Tetrabenazine 64-77 solute carrier family 18 member A2 Homo sapiens 57-62 20442355-9 2010 Tetrabenazine is extensively metabolized hepatically by the CYP2D6 enzyme to its primary active metabolite, alpha-dihydrotetrabenazine. Tetrabenazine 0-13 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 60-66 20447551-2 2010 C-11- and F-18-labeled tetrabenazine derivatives targeting VMAT2 have shown some promising results as potential biomarkers for BCM. Tetrabenazine 23-36 solute carrier family 18 member A2 Rattus norvegicus 59-64 20420689-4 2010 A specific inhibitor of vesicular monoamine transporter (VMAT2) tetrabenazine (TBZ) has been recently approved by Food and Drug Administration for treatment of HD patients in the USA. Tetrabenazine 79-82 solute carrier family 18 member A2 Homo sapiens 57-62 20560567-3 2009 The exo,exo analogue 2 had comparable affinity to lobelane and had greater affinity than the endo,endo analogue 3 at the tetrabenazine binding site on VMAT2, indicating that the preferred binding mode of lobelane is likely the extended conformation. Tetrabenazine 121-134 solute carrier family 18 member A2 Homo sapiens 151-156 20007701-5 2010 This expression system allowed identification of a new substrate, acriflavine, and isolation of mutants with modified affinity to tetrabenazine (TBZ), a non-competitive inhibitor of VMAT2 that is used in the treatment of various movement disorders including Tourette syndrome and Huntington chorea. Tetrabenazine 130-143 solute carrier family 18 member A2 Rattus norvegicus 182-187 20007701-5 2010 This expression system allowed identification of a new substrate, acriflavine, and isolation of mutants with modified affinity to tetrabenazine (TBZ), a non-competitive inhibitor of VMAT2 that is used in the treatment of various movement disorders including Tourette syndrome and Huntington chorea. Tetrabenazine 145-148 solute carrier family 18 member A2 Rattus norvegicus 182-187 20007701-8 2010 The work described here shows that in the case of rVMAT2, loss of traits acquired in evolution of function (such as serotonin transport and TBZ binding) bring about an improvement in older functions such as resistance to toxic compounds. Tetrabenazine 140-143 solute carrier family 18 member A2 Rattus norvegicus 50-56 20080893-2 2010 METHODS: In this study, a novel (18)F-labeled tetrabenazine derivative, (18)F-(+)fluoropropyldihydrotetrabenazine ((18)F-AV-133), was used for the noninvasive assessment of the vesicular monoamine transporters type 2 (VMAT2) in 17 Parkinson disease (PD) patients and 6 healthy controls. Tetrabenazine 46-59 solute carrier family 18 member A2 Homo sapiens 177-216 20080893-2 2010 METHODS: In this study, a novel (18)F-labeled tetrabenazine derivative, (18)F-(+)fluoropropyldihydrotetrabenazine ((18)F-AV-133), was used for the noninvasive assessment of the vesicular monoamine transporters type 2 (VMAT2) in 17 Parkinson disease (PD) patients and 6 healthy controls. Tetrabenazine 46-59 solute carrier family 18 member A2 Homo sapiens 218-223 17383572-7 2007 The binding of [(18)F]FP-(+)-DTBZ to the VMAT2 was shown to be reversible by administration of a competing dose of unlabeled tetrabenazine. Tetrabenazine 125-138 solute carrier family 18 member A2 Rattus norvegicus 41-46 18577569-0 2008 Role of vesicular monoamine transporter type 2 in rodent insulin secretion and glucose metabolism revealed by its specific antagonist tetrabenazine. Tetrabenazine 134-147 solute carrier family 18 member A2 Rattus norvegicus 8-46 18577569-5 2008 Using a VMAT2-specific antagonist, tetrabenazine (TBZ), we studied glucose homeostasis, insulin secretion both in vivo and ex vivo in cultures of purified rodent islets. Tetrabenazine 35-48 solute carrier family 18 member A2 Rattus norvegicus 8-13 18577569-5 2008 Using a VMAT2-specific antagonist, tetrabenazine (TBZ), we studied glucose homeostasis, insulin secretion both in vivo and ex vivo in cultures of purified rodent islets. Tetrabenazine 50-53 solute carrier family 18 member A2 Rattus norvegicus 8-13 17559790-1 2007 Two iodophenylazide derivatives of reserpine and one iodophenylazide derivative of tetrabenazine have been synthesized and characterized as photoaffinity labels of the vesicle monoamine transporter (VMAT2). Tetrabenazine 83-96 solute carrier family 18 member A2 Homo sapiens 199-204 17559790-8 2007 Incubation of [125I]TBZ-AIPP-photolabeled chromaffin granule membranes in the presence of the glycosidase N-glycanase shifted the apparent molecular weight of VMAT2 to approximately 51 kDa. Tetrabenazine 20-23 solute carrier family 18 member A2 Homo sapiens 159-164 19052001-1 2008 Tetrabenazine inhibits the transport of a molecule called vesicular monoamine transporter type 2 or VMAT2. Tetrabenazine 0-13 solute carrier family 18 member A2 Homo sapiens 100-105 18248620-6 2008 Augmented effects of alpha-methyl-para-tyrosine (alphaMT, an inhibitor of TH) and tetrabenazine (VMAT2 blocker) on DA levels suggest that also storage of DA is increased in MEN2B mice. Tetrabenazine 82-95 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 97-102 18771016-7 2008 Since the activation of the cortical neurons via the noradrenergic neurons in the brain stem is sine qua non for the acquisition for a CAR, rats treated with tetrabenazine are unable to learn in the shuttle box. Tetrabenazine 158-171 nuclear receptor subfamily 1, group I, member 3 Rattus norvegicus 135-138 18771016-8 2008 To block the activity of MAO-A (clorgyline) or to treat rats with an enhancer substance [(-)-BPAP] are the two possibilities to antagonize the learning deficit caused by tetrabenazine. Tetrabenazine 170-183 monoamine oxidase A Rattus norvegicus 25-30 18771016-12 2008 J-508 and rasagiline proved to be devoid of the enhancer property and in doses which are known to block MAO-A, they antagonized the effect of tetrabenazine, like clorgyline. Tetrabenazine 142-155 monoamine oxidase A Rattus norvegicus 104-109 17766642-2 2007 Based on our previous studies using photoaffinity-labeling techniques in characterizing the VMAT2-specific ligands ketanserin and tetrabenazine, this study describes the synthesis and characterization of a fluorenone-based compound, iodoaminoflisopolol (IAmF), as a photoprobe to identify the substrate binding site(s) of VMAT2. Tetrabenazine 130-143 solute carrier family 18 member A2 Homo sapiens 92-97 17766642-7 2007 Sf9 vesicles expressing VMAT2 show reserpine- and tetrabenazine-protectable photolabeling by [125I]IAmF. Tetrabenazine 50-63 solute carrier family 18 member A2 Homo sapiens 24-29 11489261-11 2001 In other studies, we demonstrated that the VMAT2 inhibitors tetrabenazine and Ro 4-1284 inhibit P-GP and that the P-GP inhibitors trans-flupentixol and quinidine inhibit VMAT2. Tetrabenazine 60-73 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 43-48 16934687-8 2006 Results of in vitro autoradiography with [(18)F]6b showed a distinct binding in the caudate putamen region consistent with the localization of VMAT2 in the mouse brain, which was blocked by nonradioactive TBZ efficiently. Tetrabenazine 205-208 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 143-148 16480775-5 2006 Vesicular DA uptake was temperature- and ATP-dependent and was blocked by the VMAT-2 inhibitor tetrabenazine. Tetrabenazine 95-108 solute carrier family 18 member A2 Rattus norvegicus 78-84 11984859-2 2002 Paired studies were done comparing baseline vs. TBZ treatment on the uptake of FDOPA, a measure of aromatic L-amino acid decarboxylase (AAAD) activity. Tetrabenazine 48-51 dopa decarboxylase Macaca mulatta 99-134 11984859-3 2002 Results show increased AAAD activity with TBZ treatment. Tetrabenazine 42-45 dopa decarboxylase Macaca mulatta 23-27 11984859-5 2002 Results also showed diminished responsivity of AAAD to TBZ challenge in aged monkey brain. Tetrabenazine 55-58 dopa decarboxylase Macaca mulatta 47-51 11841781-5 2002 Reevaluation of the mechanism by which lobeline alters dopamine function reveals that its primary mechanism is inhibition of dopamine uptake and promotion of dopamine release from the storage vesicles within the presynaptic terminal, via an interaction with the tetrabenazine-binding site on the vesicular monoamine transporter (VMAT2). Tetrabenazine 262-275 solute carrier family 18 member A2 Rattus norvegicus 329-334 14757360-6 2004 Transport by rVMAT2-I483A/L484A-injected oocytes was reduced to control levels by tetrabenazine, a known inhibitor of VMAT transport activity. Tetrabenazine 82-95 solute carrier family 18 member A2 Rattus norvegicus 13-19 11669473-11 2001 Only the VMAT2 blockers tetrabenazine and reserpine inhibited [3H]TBZOH specific binding. Tetrabenazine 24-37 solute carrier family 18 member A2 Homo sapiens 9-14 11489261-11 2001 In other studies, we demonstrated that the VMAT2 inhibitors tetrabenazine and Ro 4-1284 inhibit P-GP and that the P-GP inhibitors trans-flupentixol and quinidine inhibit VMAT2. Tetrabenazine 60-73 phosphoglycolate phosphatase Mus musculus 96-100 11375404-0 2001 Mutagenesis and derivatization of human vesicle monoamine transporter 2 (VMAT2) cysteines identifies transporter domains involved in tetrabenazine binding and substrate transport. Tetrabenazine 133-146 solute carrier family 18 member A2 Homo sapiens 40-71 11375404-0 2001 Mutagenesis and derivatization of human vesicle monoamine transporter 2 (VMAT2) cysteines identifies transporter domains involved in tetrabenazine binding and substrate transport. Tetrabenazine 133-146 solute carrier family 18 member A2 Homo sapiens 73-78 10415365-0 1999 Ketanserin and tetrabenazine abolish aggression in mice lacking monoamine oxidase A. Tetrabenazine 15-28 monoamine oxidase A Mus musculus 64-83 10415365-3 1999 Our results show that ketanserin and tetrabenazine (TBZ) strikingly abolished the aggressive behavior of MAO A-deficient mice. Tetrabenazine 37-50 monoamine oxidase A Mus musculus 105-110 10415365-3 1999 Our results show that ketanserin and tetrabenazine (TBZ) strikingly abolished the aggressive behavior of MAO A-deficient mice. Tetrabenazine 52-55 monoamine oxidase A Mus musculus 105-110 10415365-6 1999 Ketanserin and TBZ are both antagonists of the vesicular monoamine transporter (VMAT2). Tetrabenazine 15-18 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 80-85 10415365-7 1999 The anti-aggressive effect of TBZ and part of the effect of ketanserin may be mediated by the VMAT2. Tetrabenazine 30-33 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 94-99 9480916-7 1998 Photoaffinity labelling of rVMAT2 by 1 nM [125I]AZIK was protectable by 10 microM tetrabenazine and 10 microM 7-aminoketanserin. Tetrabenazine 82-95 solute carrier family 18 member A2 Rattus norvegicus 27-33 9325342-4 1997 Both [125I]AZIK and [125I]TBZ-AIPP photoaffinity labeling of purified rVMAT2 were protectable by 10 microM tetrabenazine (TBZ), 10 microM 7-aminoketanserin, and 1 mM concentrations of the transporter substrates dopamine, norepinephrine, and serotonin. Tetrabenazine 107-120 solute carrier family 18 member A2 Rattus norvegicus 70-76 9461580-2 1998 The neuronal VMAT2 exhibits a higher affinity for monoamine substrates and in particular for histamine as well as a greater sensitivity to the inhibitor tetrabenazine than the nonneuronal VMAT1. Tetrabenazine 153-166 solute carrier family 18 member A2 Homo sapiens 13-18 9461580-4 1998 Using site-directed mutagenesis to replace residues in TMD5-8 of VMAT2 with the equivalent residues from VMAT1, we now show that the sensitivity of VMAT2 to tetrabenazine requires Ala-315, and this interaction occurs independently of the interaction with residues in TMD9-12. Tetrabenazine 157-170 solute carrier family 18 member A2 Homo sapiens 65-70 9461580-4 1998 Using site-directed mutagenesis to replace residues in TMD5-8 of VMAT2 with the equivalent residues from VMAT1, we now show that the sensitivity of VMAT2 to tetrabenazine requires Ala-315, and this interaction occurs independently of the interaction with residues in TMD9-12. Tetrabenazine 157-170 solute carrier family 18 member A1 Homo sapiens 105-110 9461580-4 1998 Using site-directed mutagenesis to replace residues in TMD5-8 of VMAT2 with the equivalent residues from VMAT1, we now show that the sensitivity of VMAT2 to tetrabenazine requires Ala-315, and this interaction occurs independently of the interaction with residues in TMD9-12. Tetrabenazine 157-170 solute carrier family 18 member A2 Homo sapiens 148-153 9325342-4 1997 Both [125I]AZIK and [125I]TBZ-AIPP photoaffinity labeling of purified rVMAT2 were protectable by 10 microM tetrabenazine (TBZ), 10 microM 7-aminoketanserin, and 1 mM concentrations of the transporter substrates dopamine, norepinephrine, and serotonin. Tetrabenazine 26-29 solute carrier family 18 member A2 Rattus norvegicus 70-76 9106255-3 1997 However, tetrabenazine is a much less potent inhibitor of transport by rVMAT1, a form of the transporter cloned from a rat pheochromocytoma (PC12) cDNA library and expressed in CHO cells. Tetrabenazine 9-22 solute carrier family 18 member A1 Rattus norvegicus 71-77 9195934-2 1997 Functional analysis has previously shown that VMAT2 has a higher affinity than VMAT1 for monoamine neurotransmitters as well as the inhibitor tetrabenazine. Tetrabenazine 142-155 solute carrier family 18 member A2 Homo sapiens 46-51 9195934-8 1997 The mutation K446Q reduced the affinity of VMAT2 for tetrabenazine and serotonin but not histamine, whereas F464Y reduced serotonin affinity and perhaps histamine recognition but not tetrabenazine sensitivity, providing more evidence for specificity. Tetrabenazine 53-66 solute carrier family 18 member A2 Homo sapiens 43-48 9195934-12 1997 Surprisingly, the residue responsible for this difference, Tyr-434, also accounts for the higher affinity interaction of VMAT2 with tetrabenazine, histamine, and serotonin. Tetrabenazine 132-145 solute carrier family 18 member A2 Homo sapiens 121-126 9106255-11 1997 These results provide direct evidence that the differential sensitivity of rat brain and adrenal catecholamine stores to depletion by tetrabenazine and its derivatives is due to a much lower affinity of rVMAT1 for these compounds, and that NGF treatment may increase levels of rVMAT1 expression in PC12 cells. Tetrabenazine 134-147 solute carrier family 18 member A1 Rattus norvegicus 203-209 9045996-4 1997 Saturation binding of [125I]TBZ in striatal membranes demonstrated a single high affinity site (Kd = 2.3 +/- 0.9 nM and Bmax = 55.5 +/- 8.1 pmol/g tissue) with a pharmacological profile (tetrabenazine > or = iodovinyltetrabenazine > ketanserin > or = reserpine > haloperidol > GBR 12909) consistent with the specific labeling of hVMAT2. Tetrabenazine 28-31 solute carrier family 18 member A2 Homo sapiens 344-350 9080483-1 1997 The recovery of in vivo binding sites for (+/-)-alpha-[11C] methoxytetrabenazine, a radioligand for the monoamine vesicular transporter (VMAT2), was determined in mouse brain at various times following a pharmacological dose of tetrabenazine. Tetrabenazine 67-80 solute carrier family 18 (vesicular monoamine), member 2 Mus musculus 137-142 8662678-0 1996 Modification of the pH profile and tetrabenazine sensitivity of rat VMAT1 by replacement of aspartate 404 with glutamate. Tetrabenazine 35-48 solute carrier family 18 member A1 Rattus norvegicus 68-73 8643547-10 1996 Reserpine and ketanserin are slightly more potent inhibitors of VMAT2-mediated transport than of VMAT1-mediated transport, whereas tetrabenazine binds to and inhibits only VMAT2. Tetrabenazine 131-144 solute carrier family 18 member A2 Homo sapiens 172-177 8621690-4 1996 Two domains of VMAT2, one extending from transmembrane domain (TMD) 5 to the beginning of TMD8 and the other from the end of TMD9 through TMD12, increase the affinity for serotonin and histamine as well as the sensitivity to tetrabenazine but only in the context of more C-terminal and more N-terminal VMAT2 sequences, respectively. Tetrabenazine 225-238 solute carrier family 18 member A2 Homo sapiens 15-20 8621690-4 1996 Two domains of VMAT2, one extending from transmembrane domain (TMD) 5 to the beginning of TMD8 and the other from the end of TMD9 through TMD12, increase the affinity for serotonin and histamine as well as the sensitivity to tetrabenazine but only in the context of more C-terminal and more N-terminal VMAT2 sequences, respectively. Tetrabenazine 225-238 solute carrier family 18 member A2 Homo sapiens 302-307 8621690-5 1996 In addition, the extreme N terminus of VMAT2 alone suffices to confer a partial increase in substrate affinity and tetrabenazine sensitivity. Tetrabenazine 115-128 solute carrier family 18 member A2 Homo sapiens 39-44 8860238-2 1995 Transport of (3)H-histamine by both VMAT1 and VMAT2 was reserpine-sensitive but only transport by VMAT2 was inhibited by tetrabenazine. Tetrabenazine 121-134 solute carrier family 18 member A2 Rattus norvegicus 98-103