2. Academic Validation
  3. 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

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

  • Bioorg Med Chem. 2008 Feb 15;16(4):1966-82. doi: 10.1016/j.bmc.2007.10.100.
Itsuro Shimada 1,  Kyoichi Maeno,  Ken-ichi Kazuta,  Hideki Kubota,  Tetsuya Kimizuka,  Yasuharu Kimura,  Ken-ichi Hatanaka,  Yuki Naitou,  Fumikazu Wanibuchi,  Shuichi Sakamoto,  Shin-ichi Tsukamoto
Affiliations

Affiliation

  • 1 Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. itsuro.shimada@jp.astellas.com
PMID: 18035544 DOI: 10.1016/j.bmc.2007.10.100
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-furo[2,3-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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