N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists

Bioorg Med Chem Lett. 2002 Jan 21;12(2):229-32. doi: 10.1016/s0960-894x(01)00723-5.

Abstract

During our efforts to develop a novel class of selective V(1A) receptor antagonists, the N-methylbenzanilide structure was applied to a 4,4-difluoro-1-benzazepine derivative, 4, which is a selective V(1A) receptor antagonist. Further structural modifications gave 16a with high V(1A) affinity and V(2)/V(1A) selectivity (K(i)=5.71 nM, V(2)/V(1A)=140) and potent V(1A) receptor antagonist activity (ID(50)=0.0080 mg/kg iv).

MeSH terms

  • Anilides / chemistry
  • Anilides / pharmacology*
  • Antidiuretic Hormone Receptor Antagonists*
  • Arginine Vasopressin / metabolism
  • Molecular Structure
  • Receptors, Vasopressin / metabolism

Substances

  • Anilides
  • Antidiuretic Hormone Receptor Antagonists
  • Receptors, Vasopressin
  • Arginine Vasopressin
  • benzanilide