Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists |
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Authors: | Shimada Itsuro Maeno Kyoichi Kazuta Ken-ichi Kubota Hideki Kimizuka Tetsuya Kimura Yasuharu Hatanaka Ken-ichi Naitou Yuki Wanibuchi Fumikazu Sakamoto Shuichi Tsukamoto Shin-ichi |
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Institution: | Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. itsuro.shimada@jp.astellas.com |
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Abstract: | A series of novel indazole derivatives were synthesized, and their structure-activity relationships examined in order to identify potent and selective 5-HT2C receptor agonists. Among these compounds, (S)-2-(7-ethyl-1H-furo2,3-g]indazol-1-yl)-1-methylethylamine (YM348) had a good in vitro profile, that is, high agonistic activity to the human 5-HT2C receptor subtype (EC50 = 1.0 nM) and high selectivity over 5-HT2A receptors. This compound was also effective in a rat penile erection model when administered p.o. |
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