Description
Pipequaline is a partial agonist of central benzodiazepine receptors (K
i = 78 nM in a radioligand binding assay). 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. Pipequaline also increases drinking in the Vogel punished drinking task indicating anxiolytic-like activity that can be reversed by the benzodiazepine receptor antagonist flumazenil .
Uses
Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].
in vivo
Intravenously administered pipequaline exerts a partial suppression of activations by kainate, glutamate and acetylcholine. Microiontophoretic applications of pipequaline reduces the neuronal activation by kainate[2]. Pipequaline produces dose-related decreases in motor activity. Pipequaline produces significant dose-related decreases in the number of head-dips made[3].
References
[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. DOI:
10.1016/0014-2999(85)90790-3[2] Debonnel G, et al. Pipequaline acts as a partial agonist of benzodiazepine receptors: an electrophysiological study in the hippocampus of the rat. Neuropharmacology. 1987 Sep;26(9):1337-42. DOI:
10.1016/0028-3908(87)90096-7
