This is a
controlled substance with associated conditions of supply; the relevent
licence/documentation from the appropriate governing body will be required.
Chemical Name:N,N,6-Trimethyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin
e-3-acetamide
Biological Activity:
Benzodiazepine agonist with high
selectivity for α1-subunit-containing
GABAA receptors (BZ/ω1 site) and very high
intrinsic activity. Ki values are 20, 400 and ³5000 nM for α1-,
α2-/α3-, and α5-containing
GABAA receptors respectively. Hypnotic that does not induce physical
dependence.
Arbilla et al (1986) High affinity [3H]zolpidem binding in the
rat brain: an imidazopyridine with agonist properties at central benzodiazepine
receptors. Eur.J.Pharmacol. 130 257. Depoortereet al
(1986) Zolpidem, a novel nonbenzodiazepine hypnotic. 1. Neuropharmacological
and behavioural effects. J.Pharmacol.Exp.Ther. 237 649. Perraultet al (1992) Lack of tolerance and physical dependence upon repeated
treatment with the novel hypnotic zolpidem. J.Pharmacol.Exp.Ther. 263
298. Crestani et al (2000) Mechanism of action of the hypnotic
zolpidem in vivo. Br.J.Pharmacol. 131 1251.
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.