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  • Title: 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.
    Author: Kondo K, Ogawa H, Yamashita H, Miyamoto H, Tanaka M, Nakaya K, Kitano K, Yamamura Y, Nakamura S, Onogawa T, Mori T, Tominaga M.
    Journal: Bioorg Med Chem; 1999 Aug; 7(8):1743-54. PubMed ID: 10482466.
    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.
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