Pipequaline

Product NamePipequaline
CAS77472-98-1
MFC22H24N2
MW316.44
EINECS
MOL File77472-98-1.mol

Chemical Properties

Boiling point	489.2±30.0 °C(Predicted)
Density	1.078±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: 10 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml
form	A crystalline solid
pka	10.60±0.10(Predicted)
color	White to off-white

Usage And Synthesis

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