Synthesis and structure–activity relationships of a series of benzazepine derivatives as 5-HT 2C receptor agonists

…, K Sugasawa, Y Kimura, K Hatanaka, Y Naitou…

Index: Shimada, Itsuro; Maeno, Kyoichi; Kondoh, Yutaka; Kaku, Hidetaka; Sugasawa, Keizo; Kimura, Yasuharu; Hatanaka, Ken-ichi; Naitou, Yuki; Wanibuchi, Fumikazu; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 6 p. 3309 - 3320

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Citation Number: 15

Abstract

To identify potent and selective 5-HT2C receptor agonists, a series of novel benzazepine derivatives were synthesized, and their structure–activity relationships examined. The compounds were evaluated for their 5-HT2C, 5-HT2A, and 5-HT2B receptor binding affinity and intrinsic activity for the 5-HT2C and 5-HT2A receptors. Among these compounds, 6, 7- dichloro-2, 3, 4, 5-tetrahydro-1H-3-benzazepine (6) was effective in a rat penile erection ...