7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist

Bioorg Med Chem. 1999 Aug;7(8):1743-54. doi: 10.1016/s0968-0896(99)00101-7.

Abstract

We previously reported a series of benzazepine derivatives as orally active nonpeptide arginine vasopressin (AVP) V2 receptor antagonists. After the lead structure OPC-31260 was structurally evaluated and optimized, the introduction of the 7-Cl moiety on the benzazepine and 2-CH3 on the aminobenzoyl moiety enhanced its oral activity. The new AVP-V2 selective antagonist OPC-41061 was determined to be a potent and orally active agent.

MeSH terms

  • Animals
  • Antidiuretic Hormone Receptor Antagonists*
  • Arginine Vasopressin / metabolism
  • Benzazepines / chemistry
  • Benzazepines / metabolism
  • Benzazepines / pharmacology*
  • Diuretics / pharmacology
  • Magnetic Resonance Spectroscopy
  • Male
  • Molecular Structure
  • Radioligand Assay
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Vasopressin / metabolism
  • Tolvaptan

Substances

  • Antidiuretic Hormone Receptor Antagonists
  • Benzazepines
  • Diuretics
  • Receptors, Vasopressin
  • Arginine Vasopressin
  • Tolvaptan