Tricyclic heteroaromatic systems. 2-Phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one: a novel benzodiazepine receptor ligand

Farmaco. 1994 Feb;49(2):89-92.

Abstract

The synthesis, unambiguous proof of structure and benzodiazepine receptor affinity and efficacy of 2-phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one 1 are reported. The in vitro biological data indicate that 1 may be the lead compound of a new class of benzodiazepine antagonist-inverse agonist ligands.

MeSH terms

  • Animals
  • Benzoxazines
  • Binding, Competitive / drug effects
  • Brain / drug effects
  • Brain / metabolism
  • Cattle
  • Crystallography, X-Ray
  • Flunitrazepam / pharmacokinetics
  • In Vitro Techniques
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Oxazines / chemical synthesis*
  • Oxazines / pharmacology
  • Receptors, GABA-A / drug effects*
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology

Substances

  • Benzoxazines
  • Ligands
  • Oxazines
  • Receptors, GABA-A
  • Triazoles
  • 2-phenyl-1,2,4-triazolo(1,5-c)(1,3)benzoxazin-5-one
  • Flunitrazepam