Pharmacological profile of the imidazopyridine zolpidem at benzodiazepine receptors and electrocorticogram in rats

Naunyn Schmiedebergs Arch Pharmacol. 1985 Sep;330(3):248-51. doi: 10.1007/BF00572441.

Abstract

Zolpidem is a novel non-benzodiazepine related hypnotic, which possesses an imidazopyridine structure. This drug has preferential affinity for the 3H-diazepam binding site in the rat cerebellum, while it is only weakly active at inhibiting 3H-Ro 5-4864 binding to the rat kidney. The potency of zolpidem at displacing 3H-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 to 3H-benzodiazepine receptors, and because it does not affect the sleep patterns.

MeSH terms

  • Animals
  • Benzodiazepines / metabolism
  • Binding, Competitive
  • Brain / metabolism
  • Electroencephalography
  • Male
  • Pyridines / metabolism
  • Pyridines / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-A / metabolism
  • Sleep / drug effects
  • Zolpidem
  • gamma-Aminobutyric Acid / pharmacology

Substances

  • Pyridines
  • Receptors, GABA-A
  • Benzodiazepines
  • gamma-Aminobutyric Acid
  • Zolpidem