Pipequaline 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

Pipequaline 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

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

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