Researches on psychotropic agents. IV. Synthesis and neuropsychopharmacological effects of 1,3,4,14 b-tetrahydro-10-methyl-2H,10H- pyrazino[2,1-d] pyrrolo[1,2-b][1,2,5]benzotriazepine and its derivatives

Farmaco. 1992 Jul-Aug;47(7-8):987-99.

Abstract

The synthesis and neuropsychopharmacological properties of new 1,3,4,14b-tetrahydro-2H,10H-pyrazino [2,1-d] pyrrolo [1,2-b] [1,2,5] benzotriazepine derivatives related to antidepressant agent aptazepine are reported. The new derivatives displayed sedative-miorelaxant activity in mice, but no significant antagonist effect on clonidine blockade of phenylquinone-induced abdominal constriction. Among test compounds 4a, 4l and 4n showed high antinociceptive effect on the hot-plate test and compound 4e protected from death and convulsion all the electroshocked animals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemical synthesis
  • Analgesics / pharmacology
  • Animals
  • Anticonvulsants / chemical synthesis
  • Anticonvulsants / pharmacology
  • Benzazepines / chemical synthesis*
  • Benzazepines / pharmacology
  • Benzoquinones
  • Clonidine / antagonists & inhibitors
  • Clonidine / pharmacology
  • Cricetinae
  • Exploratory Behavior / drug effects
  • Female
  • Male
  • Mice
  • Motor Activity / drug effects
  • Muscle Relaxants, Central / chemical synthesis
  • Muscle Relaxants, Central / pharmacology
  • Pain / chemically induced
  • Psychotropic Drugs / chemical synthesis*
  • Psychotropic Drugs / pharmacology
  • Spectrophotometry, Infrared

Substances

  • Analgesics
  • Anticonvulsants
  • Benzazepines
  • Benzoquinones
  • Muscle Relaxants, Central
  • Psychotropic Drugs
  • phenylbenzoquinone
  • Clonidine