Summary
Zolpidem is a novel non-benzodiazepine related hypnotic, which possesses an imidazopyridine structure. This drug has preferential affinity for the3H-diazepam binding site in the rat cerebellum, while it is only weakly active at inhibiting3H-Ro 5-4864 binding to the rat kidney. The potency of zolpidem at displacing3H-Ro 15-1788 binding to rat cerebral cortex membranes is enhanced in the presence of GABA. On the sleep pattern of the electrocorticogram in the curarised rat, zolpidem induces a physiological type of slow wave sleep with rapid onset of action. Zolpidem differs from classical benzodiazepine drugs, in possessing an atypical binding profile to3H-benzodiazepine receptors, and because it does not affect the sleep patterns.
References
Braestrup C, Nielsen M (1980) Multiple benzodiazepine receptors. Trends Neurosci 3:301–303
Braestrup C, Schmiechen R, Neff G, Nielsen M, Petersen EN (1982) Interaction of convulsive ligands with benzodiazepine receptors. Science 216:1241–1243
Briley MS, Langer SZ (1978) Influence of GABA receptor agonists and antagonists on the binding of3H-diazepam to the benzodiazepine receptor. Eur J Pharmacol 52:129–132
Depoortere H (1980) Some aspects of the polygraphic studies on sleep-wakefulness cycle in rat. Waking and Sleeping 4:47–62
Depoortere H (1985) A comparative EEG study of some benzodiazepine (BZD) and non-BZD sedative or hypnotic drugs. Pharmacopsychiatr 18:17–19
Depoortere H, Decobert M, Honoré L (1983) Drug effects on the EEG of various species of laboratory animals. Neuropsychobiology 9:244–249
Karobath M, Sperk G (1979) Stimulation of benzodiazepine receptor binding by γ-aminobutyric acid. Proc Natl Acad Sci USA 76:1004–1006
Möhler H, Okada T (1977) Benzodiazepine receptor: demonstration in the central nervous system. Science (Wash. DC) 198: 849–850
Möhler H, Richards JG (1981) Agonist and antagonist benzodiazepine receptor interaction in vitro. Nature 294:763–765
Nicholson AN, Pascoe DA (1985) Hypnotic activity of an imidazopyridine (SL 80.0750). Br J Pharmacol (in press)
Nielsen M, Braestrup C (1980) Ethyl-β-carboline-3-carboxylate shows differential benzodiazepine receptor interaction. Nature 286:606–607
Regan JW, Yamamura HI, Yamada S, Roeske WR (1981) Renal benzodiazepine binding increases during deoxycorticosterone/salt hypertension in rats. Eur J Pharmacol 67:167–168
Schoemaker H, Boles RG, Horst WD, Yamamura HI (1983) Specific high affinity binding sites for [3H]Ro 5-4864 in rat brain and kidney. J Pharmacol Exp Ther 225:61–69
Sieghart W, Schuster A (1984) Affinity of various ligands for benzodiazepine receptors in the rat cerebellum and hippocampus. Biochem Pharmacol 33:4033–4038
Squires RF, Braestrup C (1977) Benzodiazepine receptors in rat brain. Nature 266:732–734
Squires RF, Benson DI, Braestrup C, Coupet, J, Klepner CA, Myers V, Beer B (1979) Some properties of brain specific benzodiazepine receptors: new evidence for multiple receptors. Pharmacol Biochem Behav 10:825–830
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Arbilla, S., Depoortere, H., George, P. et al. Pharmacological profile of the imidazopyridine zolpidem at benzodiazepine receptors and electrocorticogram in rats. Naunyn-Schmiedeberg's Arch. Pharmacol. 330, 248–251 (1985). https://doi.org/10.1007/BF00572441
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00572441