Ocinaplon

Ocinaplon is a GABA_A receptor allosteric agonist.¹ It potentiates GABA-induced currents in X. laevis oocytes expressing α₁β₂γ₂, α₂β₂γ₂, α₃β₂γ₂, and α₅β₂γ₂ subunit-containing recombinant GABA_A receptors (EC₅₀s = 3.07, 3.39, 4.59, and 3.79 µM, respectively). Ocinaplon increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, in rats with a minimum effective dose (MED) of 3.1 mg/kg. It decreases clonic convulsions induced by pentylenetetrazole (Item No. 18682) in rats (ED₅₀ = 7.5 mg/kg). Ocinaplon increases punished responding in a squirrel monkey conflict test (MED = 4 mg/kg).

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1. Lippa, A., Czobor, P., Stark, J., et al. Selective anxiolysis produced by ocinaplon, a GABA_A receptor modulator. Proc. Natl. Acad. Sci. USA 102(20), 7380-7385 (2005).