Imidazenil 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.
Imidazenil is a highly potent benzodiazepine receptor partial agonist 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 effects. In fact, imidazenil blocks the sedative effects of diazepam, yet without lowering the convulsion threshold, 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, a potent yet non-sedating anticonvulsant which might be particularly useful in the treatment of poisoning with organophosphate nerve agents, and as a novel treatment for schizophrenia.
- ^ US Patent 5317018
- ^ Thompson, D. M.; Auta, J.; Guidotti, A.; Costa, E. (1995-06-01). "Imidazenil, a new anxiolytic and anticonvulsant drug, attenuates a benzodiazepine-induced cognition deficit in monkeys". The Journal of Pharmacology and Experimental Therapeutics. 273 (3): 1307–1312. ISSN 0022-3565. PMID 7791102.
- ^ 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.
- ^ 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. 2005 Jul;180(2):191-205.