Determination of biological activity of adinazolam and its metabolites

J Pharm Pharmacol. 1984 Aug;36(8):546-8. doi: 10.1111/j.2042-7158.1984.tb04449.x.

Abstract

Adinazolam and its metabolites inhibit [3H]flunitrazepam binding in-vitro. The binding affinities of these compounds is significantly enhanced in the presence of 10-5 M muscimol, indicating that both adinazolam and its metabolites are benzodiazepine agonists. In-vivo metabolism of adinazolam results in the formation of active metabolites.

MeSH terms

  • Animals
  • Anti-Anxiety Agents / metabolism
  • Anti-Anxiety Agents / pharmacology*
  • Benzodiazepines / metabolism
  • Benzodiazepines / pharmacology*
  • Bicuculline / pharmacology
  • Brain / metabolism*
  • Cell Membrane / metabolism
  • Flunitrazepam / metabolism
  • In Vitro Techniques
  • Male
  • Muscimol / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / metabolism

Substances

  • Anti-Anxiety Agents
  • Receptors, GABA-A
  • Benzodiazepines
  • Muscimol
  • Flunitrazepam
  • adinazolam
  • Bicuculline