Title of article :
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 Original Research Article
Author/Authors :
Kazumi Kondo، نويسنده , , Hidenori Ogawa، نويسنده , , Hiroshi Yamashita، نويسنده , , Hisashi Miyamoto، نويسنده , , Michinori Tanaka، نويسنده , , Kenji Nakaya، نويسنده , , Kazuyoshi Kitano، نويسنده , , Yoshitaka Yamamura، نويسنده , , Shigeki Nakamura، نويسنده , , Toshiyuki Onogawa، نويسنده , , Toyoki Mori، نويسنده , , Michiaki Tominaga، نويسنده ,
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.
Keywords :
aquaretic , nonpeptide , orally active , Avp V2 antagonist
