- Ocinaplon
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Ocinaplon Systematic (IUPAC) name pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone Clinical data Pregnancy cat. ? Legal status ? Identifiers CAS number 96604-21-6 ATC code None PubChem CID 216456 ChemSpider 187602 UNII 2H6KVC5E76 KEGG D02617 Chemical data Formula C17H11N5O Mol. mass 301.302 g/mol SMILES eMolecules & PubChem (what is this?) (verify) Ocinaplon is an anxiolytic drug in the pyrazolopyrimidine family of drugs. Other pyrazolopyrimidine drugs include zaleplon and indiplon.
Ocinaplon has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and relatively little sedative or amnestic effect.[1]
Mechanism of action
The mechanism of action by which ocinaplon produces its anxiolytic effects is by modulating GABAA receptors,[2] although ocinaplon is more subtype-selective than most benzodiazepines.[3]
Availability
Development of ocinaplon is discontinued due to liver complications that occurred in one of the Phase III subjects.[4] However new compounds are under preclinical pipeline.[5]
References
- ^ Lippa A, Czobor P, Stark J, Beer B, Kostakis E, Gravielle M, Bandyopadhyay S, Russek SJ, Gibbs TT, Farb DH, Skolnick P. Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator. Proc Natl Acad Sci U S A. 2005 May 17;102(20):7380-5.
- ^ Mirza NR, Rodgers RJ, Mathiasen LS. Comparative cue generalization profiles of L-838, 417, SL651498, zolpidem, CL218,872, ocinaplon, bretazenil, zopiclone, and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination. J Pharmacol Exp Ther. 2006 Mar;316(3):1291-9.
- ^ Atack JR. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18.
- ^ DOV Pharmaceuticals discontinues development of ocinaplon for GAD [Anxiety Insights]
- ^ www.dovpharm.com/sub_page/products_body.html
Categories:- Pyrazolopyrimidines
- Sedatives
- Pyridines
- Ketones
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