PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 23936743-6 2013 Medicinal compounds like Ortho-7, Dibucaine and HI-6 are predicted as good targets for modeled AChE and BChE proteins based on docking studies. asoxime chloride 48-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 95-99 23917882-0 2013 Acetylcholinesterase reactivators (HI-6, obidoxime, trimedoxime, K027, K075, K127, K203, K282): structural evaluation of human serum albumin binding and absorption kinetics. asoxime chloride 35-39 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-20 23111374-6 2013 Regarding the reactivation of VX-inhibited hAChE, all compounds show a better reactivation potency than those of 2-PAM, nevertheless they are less efficient than obidoxime and HI-6. asoxime chloride 176-180 acetylcholinesterase (Cartwright blood group) Homo sapiens 43-48 23376121-0 2013 Catalytic-site conformational equilibrium in nerve-agent adducts of acetylcholinesterase: possible implications for the HI-6 antidote substrate specificity. asoxime chloride 120-124 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-88 23376121-5 2013 The interaction between HI-6 and tabun-adducts of AChE were subsequently investigated using a combination of time resolved fluorescence spectroscopy and X-ray crystallography. asoxime chloride 24-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 23376121-6 2013 Our findings show that HI-6 binds to tabun inhibited Homo sapiens AChE (hAChE) with an IC50 value of 300muM and suggest that the reactive nucleophilic moiety of HI-6 is excluded from the phosphorus atom of tabun. asoxime chloride 23-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 23376121-6 2013 Our findings show that HI-6 binds to tabun inhibited Homo sapiens AChE (hAChE) with an IC50 value of 300muM and suggest that the reactive nucleophilic moiety of HI-6 is excluded from the phosphorus atom of tabun. asoxime chloride 23-27 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-77 23376121-6 2013 Our findings show that HI-6 binds to tabun inhibited Homo sapiens AChE (hAChE) with an IC50 value of 300muM and suggest that the reactive nucleophilic moiety of HI-6 is excluded from the phosphorus atom of tabun. asoxime chloride 161-165 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 23376121-6 2013 Our findings show that HI-6 binds to tabun inhibited Homo sapiens AChE (hAChE) with an IC50 value of 300muM and suggest that the reactive nucleophilic moiety of HI-6 is excluded from the phosphorus atom of tabun. asoxime chloride 161-165 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-77 22982773-2 2013 Rate constants for reactivation of OP-inhibited AChE by even the best oximes, such as HI-6 and obidoxime, can vary >100-fold between OP-AChE conjugates that are easily reactivated and those that are difficult to reactivate. asoxime chloride 86-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 22982773-2 2013 Rate constants for reactivation of OP-inhibited AChE by even the best oximes, such as HI-6 and obidoxime, can vary >100-fold between OP-AChE conjugates that are easily reactivated and those that are difficult to reactivate. asoxime chloride 86-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 21673941-1 2011 We have in vitro tested the ability of common, commercially available, cholinesterase reactivators (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) to reactivate human acetylcholinesterase (AChE), inhibited by five structurally different organophosphate pesticides and inhibitors (paraoxon, dichlorvos, DFP, leptophos-oxon and methamidophos). asoxime chloride 151-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 177-197 22447833-1 2012 Oxime HI-6 is an efficient reactivator of the acetylcholinesterase inhibited by organophosphorous nerve agents. asoxime chloride 6-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-66 23030612-7 2012 Presently, a combination of an antimuscarinic agent, e.g. atropine, AChE reactivator such as one of the standard pyridinium oximes (pralidoxime, trimedoxime, obidoxime, HI-6) and diazepam are used for the treatment of organophosphate poisoning in humans. asoxime chloride 169-173 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 21803135-6 2011 30 muM HI 6 resulted in an almost complete recovery of sarin blocked muscle force and in an increase of completely inhibited muscle AChE activity to approx. asoxime chloride 7-11 acetylcholinesterase (Cartwright blood group) Homo sapiens 132-136 21730071-6 2011 With the most efficient human AChE mutant Y337A/F338A, we show enhanced reactivation rates for several OP-hAChE conjugates compared with wild-type hAChE when reactivated with HI-6 (1-(2"-hydroxyiminomethyl-1"-pyridinium)-3-(4"-carbamoyl-1-pyridinium)). asoxime chloride 175-179 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 20027669-5 2011 Commercial AChE reactivators (e.g. pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) were originally developed for other members of the organophosphate family, such as nerve agents (e.g. sarin, soman, tabun, VX). asoxime chloride 48-52 acetylcholinesterase (Cartwright blood group) Homo sapiens 11-15 20027669-6 2011 Pralidoxime, HI-6, and methoxime were found to be weak reactivators of OPP-inhibited AChE. asoxime chloride 13-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 22360473-7 2012 The current treatment for OPNA poisoning combines an antimuscarinic drug (e.g., atropine), an anticonvulsant drug (e.g., diazepam), and an AChE reactivator of the pyridinium aldoxime family (pralidoxime, trimedoxime, obidoxime, HI-6, HLo-7). asoxime chloride 228-232 acetylcholinesterase (Cartwright blood group) Homo sapiens 139-143 21451868-2 2011 Herein, we describe two first extremely promising uncharged reactivators for poisoned human AChE with a superior or similar in vitro ability to reactivate the enzyme as compared to that of HI-6, obidoxime, TMB-4 and HLo-7. asoxime chloride 189-193 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 21673941-1 2011 We have in vitro tested the ability of common, commercially available, cholinesterase reactivators (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) to reactivate human acetylcholinesterase (AChE), inhibited by five structurally different organophosphate pesticides and inhibitors (paraoxon, dichlorvos, DFP, leptophos-oxon and methamidophos). asoxime chloride 151-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 199-203 19663821-5 2009 Both HI-6 and irinotecan inhibited ChE/AChE activity but showed different levels of ChE inhibition in plasma and AChE inhibition in the liver and brain tissue. asoxime chloride 5-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 39-43 20888357-8 2010 Due to the high reactivity of MMB-4 a rapid reactivation of inhibited AChE can be anticipated at adequate oxime concentrations which are substantially higher compared to HI-6. asoxime chloride 170-174 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 20655881-6 2010 A homology model for wild-type Bo AChE was built using the recently published crystal structure of human AChE and used to generate models of 2-PAM and HI-6 bound to the active-sites of GF- and VR-inhibited Bo AChEs before nucleophilic attack. asoxime chloride 151-155 acetylcholinesterase (Cartwright blood group) Homo sapiens 105-109 20417629-1 2010 Catalytic activity of acetylcholinesterase (AChE; EC 3.1.1.7) was studied in the presence of oximes HI-6, K114, K127 and K203, and inhibition constants were determined for the reversible enzyme-inhibitor complex (K(I)). asoxime chloride 100-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-42 20417629-1 2010 Catalytic activity of acetylcholinesterase (AChE; EC 3.1.1.7) was studied in the presence of oximes HI-6, K114, K127 and K203, and inhibition constants were determined for the reversible enzyme-inhibitor complex (K(I)). asoxime chloride 100-104 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-48 19663821-5 2009 Both HI-6 and irinotecan inhibited ChE/AChE activity but showed different levels of ChE inhibition in plasma and AChE inhibition in the liver and brain tissue. asoxime chloride 5-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-117 20020898-1 2008 ABSTRACT This study describes the evaluation of the in vitro ability of two acetylcholinesterase (EC 3.1.1.7) reactivators, HI-6 and HLo-7, very promising at present, to reactivate human brain cholinesterases inhibited by the nerve agent cyclosarin. asoxime chloride 124-128 acetylcholinesterase (Cartwright blood group) Homo sapiens 76-96 19651196-9 2009 Presently, a combination of an antimuscarinic agent, e.g. atropine, AChE reactivator such as one of the recommended pyridinium oximes (pralidoxime, trimedoxime, obidoxime and HI-6) and diazepam are used for the treatment of OP poisoning in humans. asoxime chloride 175-179 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 19429253-7 2009 Pentylsarin-inhibited AChE could be reactivated by oximes, HI 6 being more potent than obidoxime. asoxime chloride 59-63 acetylcholinesterase (Cartwright blood group) Homo sapiens 22-26 19356117-0 2009 Study of efficacy of reactivator HI 6 in reactivation of immobilized acetylcholinesterase, inhibited by organophosphorus chemical warfare agents of the "G" series. asoxime chloride 33-37 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-89 19761810-3 2009 To investigate HI-6, K027 and HLo-7, residues lining the active-site gorge of hAChE were substituted and the effects on kinetic parameters for reactivation were determined. asoxime chloride 15-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-83 19519385-8 2009 Presently, a combination of an antimuscarinic agent, e.g. atropine, AChE reactivator such as one of the standard pyridinium oximes (pralidoxime, trimedoxime, obidoxime, HI-6) and diazepam has been used for the treatment of organophosphate poisoning in humans. asoxime chloride 169-173 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 18804659-8 2008 The most significant identification was based on methamidophos inhibited AChE reactivation by HI-6 or pralidoxime and paraoxon-ethyl inhibited AChE by obidoxime; moreover, identification of trichlorfon and paraoxon-methyl was possible, too. asoxime chloride 94-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 73-77 17370251-0 2007 Reactivation of organophosphate-inhibited human AChE by combinations of obidoxime and HI 6 in vitro. asoxime chloride 86-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 48-52 17370251-5 2007 In order to investigate the feasibility of combining obidoxime and HI 6, human AChE inhibited by sarin, cyclosarin, VX, tabun and paraoxon was reactivated by these oximes either alone or in combination. asoxime chloride 67-71 acetylcholinesterase (Cartwright blood group) Homo sapiens 79-83 17900152-8 2007 The most significant enhancement was observed in the reactivation of human AChE inhibited by nerve agents containing bulky side chains GF, GD, and VR, by H-series oximes HLo-7, HI-6, and ICD-585. asoxime chloride 177-181 acetylcholinesterase (Cartwright blood group) Homo sapiens 75-79 17913691-8 2007 After administration of HI-6, RBC-AChE activity increased rapidly. asoxime chloride 24-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-38 18254274-0 2007 Evaluation of potency of known oximes (pralidoxime, trimedoxime, HI-6, methoxime, obidoxime) to in vitro reactivate acetylcholinesterase inhibited by pesticides (chlorpyrifos and methylchlorpyrifos) and nerve agent (Russian VX). asoxime chloride 65-69 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-136 17713603-5 2007 HI-6 was effective in protection of AChE and increased its activity up to 30%; the residual activity after irinotecan inhibition was 7%. asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 36-40 18254274-5 2007 In this study, five commonly used AChE reactivators (pralidoxime, methoxime, HI-6, obidoxime, trimedoxime) for the reactivation of AChE inhibited by two pesticides (chlorpyrifos and methylchlorpyrifos) were used. asoxime chloride 77-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 34-38 18254274-5 2007 In this study, five commonly used AChE reactivators (pralidoxime, methoxime, HI-6, obidoxime, trimedoxime) for the reactivation of AChE inhibited by two pesticides (chlorpyrifos and methylchlorpyrifos) were used. asoxime chloride 77-81 acetylcholinesterase (Cartwright blood group) Homo sapiens 131-135 17252938-9 2006 Two AChE reactivators, K027 and K033, achieved comparable reactivation potency as HI-6. asoxime chloride 82-86 acetylcholinesterase (Cartwright blood group) Homo sapiens 4-8 17288495-10 2006 The article also discusses the possibility of successful therapy with HI-6 against poisoning in humans relative to doses used in non-human primates and relative to its ability to reactivate inhibited human AChE. asoxime chloride 70-74 acetylcholinesterase (Cartwright blood group) Homo sapiens 206-210 18072133-6 2006 However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10(-4) M and lower). asoxime chloride 15-19 acetylcholinesterase (Cartwright blood group) Homo sapiens 66-70 16740352-5 2006 On the base of species-specific kinetic data this model was used to calculate AChE activities in humans and pigs after percutaneous exposure to 5 x LD50 VX and treatment with HI 6. asoxime chloride 175-179 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-82 16429518-1 2005 The aim of this work was the comparison of reactivation potency of four oxime acetylcholinesterase (AChE) reactivators (pralidoxime, HI-6, K027 and K033) on three resources of the enzyme (human, pig and rat brain homogenate) inhibited by nerve agent sarin. asoxime chloride 133-137 acetylcholinesterase (Cartwright blood group) Homo sapiens 78-98 16429518-1 2005 The aim of this work was the comparison of reactivation potency of four oxime acetylcholinesterase (AChE) reactivators (pralidoxime, HI-6, K027 and K033) on three resources of the enzyme (human, pig and rat brain homogenate) inhibited by nerve agent sarin. asoxime chloride 133-137 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-104 16124202-3 2005 AChE reactivators (pralidoxime, obidoxime and HI-6) as causal antidotes are used for the cleavage of the bond between the enzyme and nerve agent. asoxime chloride 46-50 acetylcholinesterase (Cartwright blood group) Homo sapiens 0-4 16119192-3 2005 Therefore, to better evaluate the efficacy of various oximes (pralidoxime, obidoxime, HI-6, K033) to reactivate brain acetylcholinesterase inhibited by sarin by in vitro methods, human, rat and pig brain acetylcholinesterase were used to calculate kinetic parameters for the reactivation. asoxime chloride 86-90 acetylcholinesterase (Cartwright blood group) Homo sapiens 118-138 20021089-3 2005 We have confirmed the fact that currently the most promising AChE reactivator, HI-6, is the most effective reactivator of sarin-inhibited AChE. asoxime chloride 79-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 61-65 20021089-3 2005 We have confirmed the fact that currently the most promising AChE reactivator, HI-6, is the most effective reactivator of sarin-inhibited AChE. asoxime chloride 79-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 138-142 20021089-4 2005 There are only three AChE reactivators-HI-6, TO033 and TO047-able to satisfactorily reactivate sarin-inhibited AChE at the concentration 10(-5) M, which is nontoxic for human use. asoxime chloride 39-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 21-25 20021089-4 2005 There are only three AChE reactivators-HI-6, TO033 and TO047-able to satisfactorily reactivate sarin-inhibited AChE at the concentration 10(-5) M, which is nontoxic for human use. asoxime chloride 39-43 acetylcholinesterase (Cartwright blood group) Homo sapiens 111-115 9587020-6 1998 Isolated human erythrocyte AChE was inhibited with soman, sarin, cyclosarin, tabun or VX for 30 min and reactivated in the absence of inhibitory activity over 5-60 min by obidoxime, pralidoxime, HI 6 or HLo 7 (10 and 30 microM). asoxime chloride 195-199 acetylcholinesterase (Cartwright blood group) Homo sapiens 27-31 11303072-7 2001 The reactivation time of HI-6 on soman-inhibited AChE was 6 +/- 2 min. asoxime chloride 25-29 acetylcholinesterase (Cartwright blood group) Homo sapiens 49-53 10801325-2 2000 We have examined the reactivation of a series of resolved enantiomeric methylphosphonate conjugates of acetylcholinesterase by two oximes, 2-pralidoxime (2-PAM) and 1-(2"-hydroxyiminomethyl-1"-pyridinium)-3-(4"-carbamoyl-1-pyridinium) (HI-6). asoxime chloride 236-240 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-123 8911635-3 1996 In spite of this drawback, oximes are worth further investigating, since recent data derived from soman or tabun lethally intoxicated non-human primates suggest that the oxime HI-6 may exert a pharmacological effect that is not related to reactivation of inhibited AChE, but still leads to survival. asoxime chloride 176-180 acetylcholinesterase (Cartwright blood group) Homo sapiens 265-269 8493783-3 1993 Also, there have been no significant differences in efficacy and speed of reactivation of acetylcholinesterase inhibited by organophosphates when HI-6 is applied in the form of permanent intravenous infusion or repeated intramuscular injections. asoxime chloride 146-150 acetylcholinesterase (Cartwright blood group) Homo sapiens 90-110 8750900-0 1995 Methantheline improves the reactivation by HI 6 of human erythrocyte acetylcholinesterase inhibited by soman in vitro. asoxime chloride 43-47 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-89 8750900-4 1995 With HI 6 alone, the portion of AChE activity which could be reactivated 25 min after the start of ageing decreased rapidly with the delay of the oxime addition (100% of the original activity at immediate addition), the half-life being approximately 2.5 min. asoxime chloride 5-9 acetylcholinesterase (Cartwright blood group) Homo sapiens 32-36 7857205-1 1994 The purpose of this study was to compare the in vitro reactivation of the various molecular forms of soman-inhibited acetylcholinesterase by oximes such as HI-6, toxogonin and PAM, in striated muscle tissue from three species-rat, monkey and human. asoxime chloride 156-160 acetylcholinesterase (Cartwright blood group) Homo sapiens 117-137 7857205-5 1994 HI-6 (Pre-Post) increased significantly the activity of soman-inhibited acetylcholinesterase in the rat, human and monkey muscle. asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 72-92 7857205-10 1994 In addition, SAD-128, a non-oxime bispyridinium compound, appeared to enhance significantly the HI-6 induced reactivation of soman-inhibited acetylcholinesterase in human but not rat striated muscle. asoxime chloride 96-100 acetylcholinesterase (Cartwright blood group) Homo sapiens 141-161 1412499-5 1992 Based on 95% confidence limits the rank order of potentiation with eel AChE was TMB-4 = Toxogonin > HS-6 = HI-6 > 2-PAM Cl. asoxime chloride 110-114 acetylcholinesterase (Cartwright blood group) Homo sapiens 71-75 2917018-5 1989 HLo-7 is also much more active than HI-6 when used as a reactivator for electric eel AChE inhibited by some N-unsubstituted derivatives of tabun. asoxime chloride 36-40 acetylcholinesterase (Cartwright blood group) Homo sapiens 85-89 1733041-2 1992 HI-6, but neither toxogonin nor PAM Cl, antagonized sarin-induced hypothermia and reactivated brain acetylcholinesterase, in particular hypothalamic acetylcholinesterase. asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 100-120 1733041-2 1992 HI-6, but neither toxogonin nor PAM Cl, antagonized sarin-induced hypothermia and reactivated brain acetylcholinesterase, in particular hypothalamic acetylcholinesterase. asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 149-169 1890690-6 1991 The oxime HI-6 reactivated soman phosphonylated enzymes to a considerably greater extent than other oximes, and FBS AChE was notably more responsive to HI-6 than to other oximes. asoxime chloride 152-156 acetylcholinesterase (Cartwright blood group) Homo sapiens 116-120 33538594-0 2021 Structural and Biochemical Insights into the Inhibition of Human Acetylcholinesterase by G-Series Nerve Agents and Subsequent Reactivation by HI-6. asoxime chloride 142-146 acetylcholinesterase (Cartwright blood group) Homo sapiens 65-85 2596267-6 1989 The results show that HI-6 can attenuate lesions only if AChE is partially reactivated and muscle fasciculations are permanently eliminated. asoxime chloride 22-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 57-61 2742504-5 1989 On the other hand, in human muscle therapeutic treatment restored only 5%, while prophylactic application of HI-6 again resulted in about 50% recovery of control AChE activity. asoxime chloride 109-113 acetylcholinesterase (Cartwright blood group) Homo sapiens 162-166 2742504-7 1989 Immediate reactivation of rapidly aging human AChE must therefore be instituted for successful protective treatment by HI-6. asoxime chloride 119-123 acetylcholinesterase (Cartwright blood group) Homo sapiens 46-50 3345199-9 1988 All effectors increased the AChE reactivatability by HI 6 when added before aging was started. asoxime chloride 53-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 28-32 3827594-1 1986 HI 6 has been shown to be efficacious in soman intoxication of laboratory animals by reactivation of acetylcholinesterase. asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 101-121 7426043-0 1980 Reactivation of acetylcholinesterase inhibited by 1,2,2"-trimethylpropyl methylphosphonofluoridate (soman) with HI-6 and related oximes. asoxime chloride 112-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 16-36 2742504-8 1989 Retardation of aging, a direct effect of SAD-128, was roughly estimated to improve reactivation by HI-6 for about 10% of control AChE activity of the human muscle. asoxime chloride 99-103 acetylcholinesterase (Cartwright blood group) Homo sapiens 129-133 33831382-7 2021 After 30 min of incubation of AChE with soman, 5 min of aging and 20 min of reactivation by asoxime (HI-6 dichloride), AChE activity was 8.1% in control medium, 30.7% and 41.9% after addition of 1 and 10 mmol/l memantine, and 16.1% after addition of 1 mmol/l Mrz 2/373. asoxime chloride 101-116 acetylcholinesterase (Cartwright blood group) Homo sapiens 119-123 33538594-7 2021 With reports indicating that the efficacy of reactivators can vary based on the nerve agent inhibiting hAChE, human recombinatorially expressed hAChE was utilized to define these variations for HI-6 among various G-agents. asoxime chloride 194-198 acetylcholinesterase (Cartwright blood group) Homo sapiens 144-149 33538594-8 2021 To identify the structural underpinnings of this phenomenon, the structures of tabun, sarin, and soman-inhibited hAChE in complex with HI-6 were determined. asoxime chloride 135-139 acetylcholinesterase (Cartwright blood group) Homo sapiens 113-118 32267631-1 2020 Oximes like pralidoxime (2-PAM), obidoxime (Obi) and HI-6 are the only currently available therapeutics to reactivate inhibited acetylcholinesterase (AChE) in case of intoxications with organophosphorus (OP) compounds. asoxime chloride 53-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-148 32267631-1 2020 Oximes like pralidoxime (2-PAM), obidoxime (Obi) and HI-6 are the only currently available therapeutics to reactivate inhibited acetylcholinesterase (AChE) in case of intoxications with organophosphorus (OP) compounds. asoxime chloride 53-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 150-154 28993240-5 2018 It turned out that only HI-6 was able to slow down the ongoing inhibition of human AChE by soman without preventing final complete inhibition of the enzyme. asoxime chloride 24-28 acetylcholinesterase (Cartwright blood group) Homo sapiens 83-87 30763608-9 2019 Both substances restored AChE activity in a dose-dependent way, with HI-6 being more potent (HI-6 EC50 = 3.8 muM vs obidoxime EC50 = 197.8 muM). asoxime chloride 69-73 acetylcholinesterase (Cartwright blood group) Homo sapiens 25-29 32175496-3 2020 HI-6 and 2-PAM are cationic oximes proved to be effective for the reactivation of AChE inhibited by the nerve agents VX and sarin (GB). asoxime chloride 0-4 acetylcholinesterase (Cartwright blood group) Homo sapiens 82-86 32175496-9 2020 In contrast, HI-6 and 2-PAM showed higher affinities with more negative binding energy values and larger contribution of the amino acid Asp74, demonstrating the importance of the quaternary nitrogen to the affinity and interaction of oximes with AChE-GB and AChE-VX conjugates. asoxime chloride 13-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 246-250 30858091-12 2019 However, the oxime HI-6 as potent reactivator of cyclosarin-inhibited AChE was not able to prevent the FPDc prolongation in this model. asoxime chloride 19-23 acetylcholinesterase (Cartwright blood group) Homo sapiens 70-74 30462502-0 2018 Structural Insights of Stereospecific Inhibition of Human Acetylcholinesterase by VX and Subsequent Reactivation by HI-6. asoxime chloride 116-120 acetylcholinesterase (Cartwright blood group) Homo sapiens 58-78 30462502-4 2018 Beyond identifying hAChE structural features that lend themselves to stereospecific inhibition, structures of the reactivator HI-6 bound to hAChE inhibited by VX enantiomers of varying toxicity, or in its uninhibited state, were obtained. asoxime chloride 126-130 acetylcholinesterase (Cartwright blood group) Homo sapiens 140-145 30312685-8 2018 A combination of 3 l and the bispyridinium oxime HI-6 was tested to reactivate OP-inhibited AChE: The superior reactivator of the respective OP-AChE combination dominated the reactivation process and a synergistic effect could not be observed. asoxime chloride 49-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 92-96 29019446-3 2018 In order to try to find out the reason for this, a computational study involving molecular docking, molecular dynamics, and binding energies calculations, was performed on the binding modes of HI-6 and HS-6 on human AChE (HssAChE) inhibited by those nerve agents. asoxime chloride 193-197 acetylcholinesterase (Cartwright blood group) Homo sapiens 216-220 28446076-0 2018 Behavior of uncharged oximes compared to HI6 and 2-PAM in the human AChE-tabun conjugate: a molecular modeling approach. asoxime chloride 41-44 acetylcholinesterase (Cartwright blood group) Homo sapiens 68-72 29773682-2 2018 To investigate oximate water structure changes in this reaction, reactivation of paraoxon-inhibited human acetylcholinesterase (AChE) was performed by the oxime asoxime (HI-6) at different pH in the presence and absence of lyotropic salts: a neutral salt (NaCl), a strong chaotropic salt (LiSCN) and strong kosmotropic salts (ammonium sulphate and phosphate HPO42-). asoxime chloride 170-174 acetylcholinesterase (Cartwright blood group) Homo sapiens 106-126 28446076-2 2018 Some oximes such HI6 as 2-PAM are nucleophiles that are capable to reactivate inhibited human AChE under some conditions. asoxime chloride 17-20 acetylcholinesterase (Cartwright blood group) Homo sapiens 94-98 28446076-7 2018 In contrast, HI 6 and 2-PAM showed high binding energy values with great contribution of the amino acid Asp74, demonstrating the importance of the quaternary nitrogen to the affinity and interaction of the oximes/AChE tabun-inhibited complexes. asoxime chloride 13-17 acetylcholinesterase (Cartwright blood group) Homo sapiens 213-217 29773682-2 2018 To investigate oximate water structure changes in this reaction, reactivation of paraoxon-inhibited human acetylcholinesterase (AChE) was performed by the oxime asoxime (HI-6) at different pH in the presence and absence of lyotropic salts: a neutral salt (NaCl), a strong chaotropic salt (LiSCN) and strong kosmotropic salts (ammonium sulphate and phosphate HPO42-). asoxime chloride 170-174 acetylcholinesterase (Cartwright blood group) Homo sapiens 128-132 29735900-2 2018 For the recovery of inhibited AChE, antidotes from the group of pyridinium or bispyridinium aldoxime reactivators (pralidoxime, obidoxime, HI-6) are used in combination with anticholinergics and anticonvulsives. asoxime chloride 139-143 acetylcholinesterase (Cartwright blood group) Homo sapiens 30-34 27153754-0 2016 Reactivation of nerve agent-inhibited human acetylcholinesterase by obidoxime, HI-6 and obidoxime+HI-6: Kinetic in vitro study with simulated nerve agent toxicokinetics and oxime pharmacokinetics. asoxime chloride 79-83 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-64 27358236-4 2017 We here semiquantitatively investigate the ability of obidoxime and HI-6 to decrease the inhibitory activity of VX with human AChE and BChE from whole blood, erythrocyte membranes, erythrocytes, plasma, clinically available fresh frozen plasma and packed red blood cells. asoxime chloride 68-72 acetylcholinesterase (Cartwright blood group) Homo sapiens 126-130 27191504-8 2016 Ternary structures of paraoxon-inhibited human acetylcholinesterase in complex with the oximes HI6 and 2-PAM reveals relatively poor positioning for reactivation. asoxime chloride 95-98 acetylcholinesterase (Cartwright blood group) Homo sapiens 47-67 27179675-7 2016 Based on the full information provided by this method, the efficacy of reactivators, such as HI-6, obidoxime and pralidoxime, in the typical treatment of NAs poisoned AChE in in vitro was further evaluated. asoxime chloride 93-97 acetylcholinesterase (Cartwright blood group) Homo sapiens 167-171 27153754-0 2016 Reactivation of nerve agent-inhibited human acetylcholinesterase by obidoxime, HI-6 and obidoxime+HI-6: Kinetic in vitro study with simulated nerve agent toxicokinetics and oxime pharmacokinetics. asoxime chloride 98-102 acetylcholinesterase (Cartwright blood group) Homo sapiens 44-64 27153754-5 2016 The oxime-induced reactivation of inhibited human AChE in the presence of nerve agents is markedly impaired and the combination of obidoxime and HI-6 had no additive effect but could broaden the spectrum. asoxime chloride 145-149 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 26468911-2 2015 We present oxime (HI-6) unbinding from the active site gorge of AChE, known to be strongly influenced by intermolecular cation-pi, hydrogen bridge (HB) and water bridge (WB) interactions and by molecular simulations with effective polarization in polarizable mean-field model of TIP3P water. asoxime chloride 18-22 acetylcholinesterase (Cartwright blood group) Homo sapiens 64-68 25240274-5 2014 Incubation of human AChE with millimolar DF and MF and subsequent addition of obidoxime and HI-6 resulted in a concentration-dependent decrease of AChE activity. asoxime chloride 92-96 acetylcholinesterase (Cartwright blood group) Homo sapiens 20-24 25240274-5 2014 Incubation of human AChE with millimolar DF and MF and subsequent addition of obidoxime and HI-6 resulted in a concentration-dependent decrease of AChE activity. asoxime chloride 92-96 acetylcholinesterase (Cartwright blood group) Homo sapiens 147-151