Pipequaline (PK-8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. Pipequaline acts as a non-selective GABAA receptor partial agonist. Pipequaline produces dose-related decreases in motor activity. Pipequaline produces significant dose-related decreases in the number of head-dips made.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 28 mg/mL|
The effects on memory of pipequaline, alone or in combination with diazepam
F F Eves, et al. Psychopharmacology (Berl). 1988;95(3):386-9. PMID: 3137626.
Effects of PK 8165, a partial benzodiazepine receptor agonist, on cholecystokinin-induced activation of hippocampal pyramidal neurons: a microiontophoretic study in the rat
J Bradwejn, et al. Eur J Pharmacol. 1985 Jun 19;112(3):415-8. PMID: 2990972.
Pipequaline acts as a partial agonist of benzodiazepine receptors: an electrophysiological study in the hippocampus of the rat
G Debonnel, et al. Neuropharmacology. 1987 Sep;26(9):1337-42. PMID: 2823163.
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