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Pipequaline is a partial agonist of central benzodiazepine receptors (Ki = 78 nM in a radioligand binding assay).1 In mice, pipequaline enhances the effects of diazepam (Item No. ISO60177), further reducing foot shock-induced fighting behavior and the number of maximal electroshock-induced seizures and potentiating the muscle relaxant and hypnotic effects.2 Pipequaline also increases drinking in the Vogel punished drinking task indicating anxiolytic-like activity that can be reversed by the benzodiazepine receptor antagonist flumazenil (Item No. 14252).
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1. Multiple benzodiazepine receptors: Evidence of a dissociation between anticonflict and anticonvulsant properties by PK 8165 and PK 9084 (two quinoline derivatives). Life Sci. 28(13), 1439-1448 (1981).
2. Pharmacological evidence that PK 8165 behaves as a partial agonist of brain type benzodiazepine receptors. Arch. Int. Pharmacodyn. Ther. 271(2), 189-197 (1984).