A partial agonist of central benzodiazepine receptors
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)
Animal experiment: | Rats: Pipequaline is dissolved in water to give injection volumes of 2 mL/kg. Rats are injected with 5, 10, and 50 mg/kg pipequaline. Infrared cells in the walls of the box provided automated measures of locomotor activity and rearing, respectively[3]. |
参考文献: [1]. Bradwejn J, et al. Effects of PK 8165, a partial benzodiazepine receptor agonist, on cholecystokinin-inducedactivation of hippocampal pyramidal neurons: a microiontophoretic study in the rat. Eur J Pharmacol. 1985 Jun 19;112(3):415-8. | |
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