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 , 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 .
1.Le Fur, G., Mizoule, J., Burgevin, M.C., et al.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.Mizoule, J., Rataud, J., Uzan, A., et al.Pharmacological evidence that PK 8165 behaves as a partial agonist of brain type benzodiazepine receptorsArch. Int. Pharmacodyn. Ther.271(2)189-197(1984)