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Ocinaplon is a GABAA receptor allosteric agonist.1 It potentiates GABA-induced currents in X. laevis oocytes expressing α1β2γ2, α2β2γ2, α3β2γ2, and α5β2γ2 subunit-containing recombinant GABAA 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).
WARNING This product is not for human or veterinary use.
1. Selective anxiolysis produced by ocinaplon, a GABAA receptor modulator. Proc. Natl. Acad. Sci. USA 102(20), 7380-7385 (2005).