Ocinaplon

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Ocinaplon
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Systematic (IUPAC) name
pyridin-2-yl-(7-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl)methanone
Identifiers
CAS Number 96604-21-6
ATC code none
PubChem CID 216456
Chemical data
Formula C17H11N5O
Molar mass 301.302 g/mol[[Script error: No such module "String".]]
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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

  1. Jump up 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. Jump up 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. Jump up 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. Jump up DOV Pharmaceuticals discontinues development of ocinaplon for GAD [Anxiety Insights]
  5. Jump up www.dovpharm.com/sub_page/products_body.html
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