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Ocinaplon
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 216456
Chemical data
Formula C 17H11N5O 
Mol. mass 301.302 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

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