Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives

J Med Chem. 1980 Aug;23(8):952-5. doi: 10.1021/jm00182a026.

Abstract

The synthesis and biological evaluation of some derivatives of pyrazino[1,2-a][1,4]benzodiazepines for anxiolytic and antidepressant activity are presented. Significant levels of anxiolytic activity were noted for 7-(o-chlorophenyl)-9-chloro-1,2,3,4,4a,5-hexahydro-3-methylpyrazino[1,2-a];E11,4]benzodiazepine (4b).

MeSH terms

  • Animals
  • Anti-Anxiety Agents / chemical synthesis
  • Anticonvulsants / chemical synthesis
  • Apomorphine / antagonists & inhibitors
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / metabolism
  • Benzodiazepines / pharmacology
  • Diazepam / metabolism
  • Guinea Pigs
  • Histamine Antagonists / chemical synthesis
  • In Vitro Techniques
  • Male
  • Norepinephrine / metabolism
  • Pyrazines / chemical synthesis
  • Pyrazines / pharmacology
  • Rats
  • Receptors, Drug / metabolism
  • Serotonin / metabolism

Substances

  • Anti-Anxiety Agents
  • Anticonvulsants
  • Histamine Antagonists
  • Pyrazines
  • Receptors, Drug
  • Benzodiazepines
  • Serotonin
  • Apomorphine
  • Diazepam
  • Norepinephrine