Ocinaplon has a similar pharmacological profile to thebenzodiazepine family of drugs, but with mainly anxiolytic properties and relatively littlesedative oramnestic effect.[1]
The mechanism of action by which ocinaplon produces its anxiolytic effects is by modulatingGABAA receptors,[3] although ocinaplon is more subtype-selective than most benzodiazepines.[4][5]
Condensation of4-Acetylpyridine[9] with N,N-Dimethylformamide dimethyl acetal (DMFDMA) gives the "enamide" (3). This is then condensed with (3-Amino-1H-pyrazol-4-yl)(2-pyridinyl)methanone (4) (96219-90-8).[10][11] This is the same intermediate as was used in the synthesis ofzaleplon in which the nitrile is replaced by a 2-acetylpyridil moiety. This affords theanxiolytic agent ocinaplon (5).
^Slee A, Nazareth I, Bondaronek P, Liu Y, Cheng Z, Freemantle N (February 2019). "Pharmacological treatments for generalised anxiety disorder: a systematic review and network meta-analysis".Lancet.393 (10173):768–777.doi:10.1016/S0140-6736(18)31793-8.PMID30712879.S2CID72332967.
^Mirza NR, Rodgers RJ, Mathiasen LS (March 2006). "Comparative cue generalization profiles of L-838, 417, SL651498, zolpidem, CL218,872, ocinaplon, bretazenil, zopiclone, and various benzodiazepines in chlordiazepoxide and zolpidem drug discrimination".The Journal of Pharmacology and Experimental Therapeutics.316 (3):1291–9.doi:10.1124/jpet.105.094003.PMID16339395.S2CID21913400.
^Atack JR (May 2005). "The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics".Expert Opinion on Investigational Drugs.14 (5):601–18.doi:10.1517/13543784.14.5.601.PMID15926867.S2CID22793644.
