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N-Tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B

✍ Scribed by Yoon Jin Kwon; Simon Saubern; James M. Macdonald; Xi-Ping Huang; Vincent Setola; Bryan L. Roth

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 237 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.074

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✦ Synopsis

The serendipitous discovery of N-cyclohexyl-8-fluoro-3,3a,4,9b-tetrahydro-1H-thiochromeno[4,3-c]isoxazole-1-carboxamide as a selective human serotonin 5-HT 2B antagonist with K i of 42 ± 5 nM is reported herein. A subsequent functional assay indicated little agonist activity compared to 5-HT itself.

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