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Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.

Pipequaline is extensively bound to plasma proteins: i.e. human serum albumin (HSA), alpha-1-acid glycoprotein (AAG), lipoproteins and blood cells, mainly erythrocytes[1].

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].

[1]. Essassi D, et al. Pipequaline transport from blood to brain and liver: role of plasma protein-bound drug. J Pharm Pharmacol. 1989 Sep;41(9):595-600. [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. [3]. File SE., et al. Sedative effects of PK 9084 and PK 8165, alone and in combination with chlordiazepoxide. Br J Pharmacol. 1983 May;79(1):219-23.

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