Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2195-8. doi: 10.1016/s0960-894x(03)00388-3.

Abstract

Novel tricyclic benzazepine derivatives were synthesized as arginine vasopressin (AVP) antagonists. Several tricyclic compounds showed potent antagonistic activity in rat AVP receptors V(1a) and V(2). Derivatives containing pyrrolo-tricyclic amines, 13i-k, 30, and 31 also showed selectivity for the V(2) receptor.

MeSH terms

  • Animals
  • Arginine Vasopressin / antagonists & inhibitors*
  • Benzazepines / chemical synthesis*
  • Benzazepines / pharmacology*
  • Dose-Response Relationship, Drug
  • Indicators and Reagents
  • Kidney Medulla / drug effects
  • Kidney Medulla / metabolism
  • Liver / drug effects
  • Liver / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
  • Urodynamics / drug effects

Substances

  • Benzazepines
  • Indicators and Reagents
  • Arginine Vasopressin