Ocinaplon

Ocinaplon is an anxiolytic drug in the pyrazolopyrimidine family of drugs. Other pyrazolopyrimidine drugs include zaleplon and indiplon.

Additional recommended knowledge

How to quickly check pipettes?

Correct Test Weight Handling Guide: 12 Practical Tips

Essential Laboratory Skills Guide

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 GABA_A receptors,^[2] although ocinaplon is more subtype-selective than most benzodiazepines.^[3]

Availability

Development of ocinaplon is discontinued ue to liver complications that occurred in one of the Phase III subjects. ^[4] However new compounds are under preclinical pipeline. ^[5]

References

1. ^ 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.
2. ^ 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.
3. ^ 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.
4. ^ http://www.anxietyinsights.info/dov_pharmaceuticals_discontinues_development_of_ocinaplon_fo.htm
5. ^ www.dovpharm.com/sub_page/products_body.html