Chemical Name:4,5-Dihydro-4,4-dimethyl-imidazo[1,5-a]quinoxaline-3-ca
rboxylic acid 1,1-dimethylethyl ester
Biological Activity:
GABAA receptor antagonist that binds
the picrotoxin site and stabilises the inactive form of the channel via
allosteric interaction. Accelerates the decay of GABA-induced Cl-
currents with little effect on peak amplitude. Also inhibits 5-HT3A
receptors via a similar mechanism.
Dillonet al
(1993) U-93631 causes rapid decay of γ-aminobutyric
acid-induced chloride currents in recombinant rat γ-aminobutyric acid type A receptors.
Mol.Pharmacol. 44 860. Dillonet al (1995)
[4-Dimethyl-3-t-butylcarboxyl-4,5-dihydro (1,5-a) quinoxaline] is a novel
ligand to the picrotoxin site on GABAA receptors, and decreases
single-channel open probability. J.Pharmacol.Exp.Ther. 272 597. Daset al (2003) The GABAA receptor antagonist picrotoxin
inhibits 5-hydroxytryptamine type 3A receptors. Neuropharmacol. 44
431.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.