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

Article abstract of DOI:10.1016/S0968-0896(99)00101-7

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. Copyright (C) 1999 Elsevier Science Ltd.