Imidazenil is a highly potent benzodiazepine receptorpartial agonist[2] with an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant and anxiolytic effects, yet without any notable sedative or amnestic[3] effects. In fact, imidazenil blocks the sedative effects of diazepam, yet without lowering the convulsion threshold,[4] and so potentially could be a more flexible antidote than the antagonist flumazenil which is commonly used to treat benzodiazepine overdose at present.
Imidazenil has not yet been developed commercially for use in humans, however it has been suggested as a safe and effective treatment for anxiety,[5] a potent yet non-sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agents,[6][7] and as a novel treatment for schizophrenia.[8]
^Thompson DM, Auta J, Guidotti A, Costa E (June 1995). "Imidazenil, a new anxiolytic and anticonvulsant drug, attenuates a benzodiazepine-induced cognition deficit in monkeys". The Journal of Pharmacology and Experimental Therapeutics. 273 (3): 1307–12. PMID 7791102.
^Auta J, Faust WB, Lambert P, Guidotti A, Costa E, Moerschbaecher JM (June 1995). "Comparison of the effects of full and partial allosteric modulators of GABA(A) receptors on complex behavioral processes in monkeys". Behavioural Pharmacology. 6 (4): 323–332. doi:10.1097/00008877-199506000-00003. PMID 11224341. S2CID 24584434.
^Auta J, Costa E, Davis JM, Guidotti A (September 2005). "Imidazenil: an antagonist of the sedative but not the anticonvulsant action of diazepam". Neuropharmacology. 49 (3): 425–9. doi:10.1016/j.neuropharm.2005.04.005. PMID 15964602. S2CID 44619421.
^Atack JR (August 2003). "Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site". Current Drug Targets. CNS and Neurological Disorders. 2 (4): 213–32. doi:10.2174/1568007033482841. PMID 12871032.
^Rump S, Gidynska T, Galecka E, Antkowiak O, Nawrocka M, Kowalczyk M (2000). "Effects of imidazenil, a new benzodiazepine receptor partial agonist, in the treatment of convulsions in organophosphate intoxications". Neurotoxicity Research. 2 (1): 17–22. doi:10.1007/bf03033323. PMID 15545002. S2CID 2066413.
^Auta J, Costa E, Davis J, Guidotti A (March 2004). "Imidazenil: a potent and safe protective agent against diisopropyl fluorophosphate toxicity". Neuropharmacology. 46 (3): 397–403. doi:10.1016/j.neuropharm.2003.09.010. PMID 14975695. S2CID 41221807.
^Guidotti A, Auta J, Davis JM, Dong E, Grayson DR, Veldic M, et al. (July 2005). "GABAergic dysfunction in schizophrenia: new treatment strategies on the horizon". Psychopharmacology. 180 (2): 191–205. doi:10.1007/s00213-005-2212-8. PMID 15864560. S2CID 25147595.
February 09, 2023
imidazenil, experimental, anxiolytic, drug, which, derived, from, benzodiazepine, family, most, closely, related, other, imidazobenzodiazepines, such, midazolam, flumazenil, bretazenil, clinical, dataatc, codenonelegal, statuslegal, statusca, schedule, ivident. Imidazenil 1 is an experimental anxiolytic drug which is derived from the benzodiazepine family and is most closely related to other imidazobenzodiazepines such as midazolam flumazenil and bretazenil ImidazenilClinical dataATC codenoneLegal statusLegal statusCA Schedule IVIdentifiersIUPAC name 6 2 Bromophenyl 8 fluoro 4H imidazo 1 5 a 1 4 benzodiazepine 3 carboxamideCAS Number151271 08 8 YPubChem CID119194ChemSpider106482 YUNII7N95V6864RCompTox Dashboard EPA DTXSID90164746Chemical and physical dataFormulaC 18H 12Br F N 4OMolar mass399 223 g mol 13D model JSmol Interactive imageSMILES Brc4ccccc4C 2 N Cc1c ncn1c3c 2cc F cc3 C O NInChI InChI 1S C18H12BrFN4O c19 13 4 2 1 3 11 13 16 12 7 10 20 5 6 14 12 24 9 23 17 18 21 25 15 24 8 22 16 h1 7 9H 8H2 H2 21 25 YKey OCJHYHKWUWSHEN UHFFFAOYSA N Y verify Imidazenil is a highly potent benzodiazepine receptor partial agonist 2 with an unusual profile of effects producing some of the effects associated with normal benzodiazepines such as anticonvulsant and anxiolytic effects yet without any notable sedative or amnestic 3 effects In fact imidazenil blocks the sedative effects of diazepam yet without lowering the convulsion threshold 4 and so potentially could be a more flexible antidote than the antagonist flumazenil which is commonly used to treat benzodiazepine overdose at present Imidazenil has not yet been developed commercially for use in humans however it has been suggested as a safe and effective treatment for anxiety 5 a potent yet non sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agents 6 7 and as a novel treatment for schizophrenia 8 See also EditFlumazenil Bretazenil GL II 73 MidazolamReferences Edit US 5317018 Thompson DM Auta J Guidotti A Costa E June 1995 Imidazenil a new anxiolytic and anticonvulsant drug attenuates a benzodiazepine induced cognition deficit in monkeys The Journal of Pharmacology and Experimental Therapeutics 273 3 1307 12 PMID 7791102 Auta J Faust WB Lambert P Guidotti A Costa E Moerschbaecher JM June 1995 Comparison of the effects of full and partial allosteric modulators of GABA A receptors on complex behavioral processes in monkeys Behavioural Pharmacology 6 4 323 332 doi 10 1097 00008877 199506000 00003 PMID 11224341 S2CID 24584434 Auta J Costa E Davis JM Guidotti A September 2005 Imidazenil an antagonist of the sedative but not the anticonvulsant action of diazepam Neuropharmacology 49 3 425 9 doi 10 1016 j neuropharm 2005 04 005 PMID 15964602 S2CID 44619421 Atack JR August 2003 Anxioselective compounds acting at the GABA A receptor benzodiazepine binding site Current Drug Targets CNS and Neurological Disorders 2 4 213 32 doi 10 2174 1568007033482841 PMID 12871032 Rump S Gidynska T Galecka E Antkowiak O Nawrocka M Kowalczyk M 2000 Effects of imidazenil a new benzodiazepine receptor partial agonist in the treatment of convulsions in organophosphate intoxications Neurotoxicity Research 2 1 17 22 doi 10 1007 bf03033323 PMID 15545002 S2CID 2066413 Auta J Costa E Davis J Guidotti A March 2004 Imidazenil a potent and safe protective agent against diisopropyl fluorophosphate toxicity Neuropharmacology 46 3 397 403 doi 10 1016 j neuropharm 2003 09 010 PMID 14975695 S2CID 41221807 Guidotti A Auta J Davis JM Dong E Grayson DR Veldic M et al July 2005 GABAergic dysfunction in schizophrenia new treatment strategies on the horizon Psychopharmacology 180 2 191 205 doi 10 1007 s00213 005 2212 8 PMID 15864560 S2CID 25147595 Retrieved from https en wikipedia org w index php title Imidazenil amp oldid 1084243649, wikipedia, wiki, book, books, library,
