Imidazenil


Imidazenil
Systematic (IUPAC) name
6-(2-bromophenyl)-8-fluoro-4H- imidazo[1,5-a][1,4]benzodiazepine-3-carboxamide
Identifiers
CAS number	151271-08-8
ATC code	?
PubChem	119194
Chemical data
O
Mol. mass	399.216 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Imidazenil is an bretazenil.

Imidazenil is a overdose at present.

This unusual profile of effects makes imidazenil potentially a very useful drug. In animal studies it has been shown to be an effective anxiolytic and strong anticonvulsant, yet without many of the side effects associated with other benzodiazepines; it does not produce tolerance^[5] or dependence,^[6] reverses the amnestic effects of conventional benzodiazepines, and does not potentiate the effects of alcohol.^[7]^[8]

Imidazenil has not yet been developed commercially for use in humans, however it has been suggested as a safe and effective treatment for anxiety,^[9] a potent yet non-sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agents,^[10]^[11] and as a novel treatment for schizophrenia.^[12]

References

^ Griebel G, Sanger DJ, Perrault G. Further evidence for differences between non-selective and BZ-1 (omega 1) selective, benzodiazepine receptor ligands in murine models of "state" and "trait" anxiety. Neuropharmacology. 1996;35(8):1081-91.
^ Giusti P, Ducic I, Puia G, Arban R, Walser A, Guidotti A, Costa E. Imidazenil: a new partial positive allosteric modulator of gamma-aminobutyric acid (GABA) action at GABAA receptors. Journal of Pharmacology and Experimental Therapeutics. 1993 Aug;266(2):1018-28.
^ Auta J, Faust WB, Lambert P, Guidotti A, Costa E, Moerschbaecher JM. Comparison of the effects of full and partial allosteric modulators of GABA(A) receptors on complex behavioral processes in monkeys. Behavioural Pharmacology. 1995 Jun;6(4):323-332.
^ Auta J, Costa E, Davis JM, Guidotti A. Imidazenil: an antagonist of the sedative but not the anticonvulsant action of diazepam. Neuropharmacology. 2005 Sep;49(3):425-9.
^ Ghiani CA, Serra M, Motzo C, Giusti P, Cuccheddu T, Porceddu ML, Biggio G. Chronic administration of an anticonvulsant dose of imidazenil fails to induce tolerance of GABAA receptor function in mice. European Journal of Pharmacology. 1994 Mar 21;254(3):299-302.
^ Auta J, Giusti P, Guidotti A, Costa E. Imidazenil, a partial positive allosteric modulator of GABAA receptors, exhibits low tolerance and dependence liabilities in the rat. Journal of Pharmacology and Experimental Therapeutics. 1994 Sep;270(3):1262-9.
^ Thompson DM, Auta J, Guidotti A, Costa E. Imidazenil, a new anxiolytic and anticonvulsant drug, attenuates a benzodiazepine-induced cognition deficit in monkeys. Journal of Pharmacology and Experimental Therapeutics. 1995 Jun;273(3):1307-12.
^ Auta J, Guidotti A, Costa E. Imidazenil prevention of alprazolam-induced acquisition deficit in patas monkeys is devoid of tolerance. Proceedings of the National Academy of Sciences U S A. 2000 Feb 29;97(5):2314-9.
^ Atack JR. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Current Drug Targets. CNS and Neurological Disorders. 2003 Aug;2(4):213-32.
^ Rump S, Gidynska T, Galecka E, Antkowiak O, Nawrocka M, Kowalczyk M. Effects of imidazenil, a new benzodiazepine receptor partial agonist, in the treatment of convulsions in organophosphate intoxications. Neurotoxicity Research. 2000;2(1):17-22.
^ Auta J, Costa E, Davis J, Guidotti A. Imidazenil: a potent and safe protective agent against diisopropyl fluorophosphate toxicity. Neuropharmacology. 2004 Mar;46(3):397-403.
^ Guidotti A, Auta J, Davis JM, Dong E, Grayson DR, Veldic M, Zhang X, Costa E. GABAergic dysfunction in schizophrenia: new treatment strategies on the horizon. Psychopharmacology (Berlin). 2005 Jul;180(2):191-205.

v • d • e N05CD)
1,4-Benzodiazepines	Bromazepam • Camazepam • Chlordiazepoxide • Cinolazepam • Clonazepam • Clorazepate • Cyprazepam • Delorazepam • Diazepam • Doxefazepam • Elfazepam • Ethyl loflazepate • Fletazepam • Fludiazepam • Fosazepam • Flunitrazepam • Flurazepam • Flutoprazepam • Gidazepam • Halazepam • Iclazepam • Lorazepam • Lormetazepam • Meclonazepam • Medazepam • Menitrazepam • Metaclazepam • Nimetazepam • Nitrazepam • Nordazepam • Oxazepam • Phenazepam • Pinazepam • Pivoxazepam • Prazepam • Quazepam • QH-II-66 • Reclazepam • Sulazepam • Temazepam • Tetrazepam • Uldazepam
Triazolobenzodiazepines	Adinazolam • Alprazolam • Estazolam • Triazolam • Zapizolam
Imidazobenzodiazepines	Bretazenil • Flumazenil • Imidazenil • Loprazolam • Midazolam • Ro15-4513
Oxazolobenzodiazepines	Cloxazolam • Flutazolam • Haloxazolam • Mexazolam • Oxazolam
Thienobenzodiazepines	Zolazepam

v • d • e Psycholeptics: Tandospirone
Other	Mephenoxalone

Benzodiazepines

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Imidazenil". A list of authors is available in Wikipedia.