N-Tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B |
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| Authors: | Yoon Jin Kwon Simon Saubern James M Macdonald Xi-Ping Huang Vincent Setola Bryan L Roth |
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| Institution: | 1. CSIRO Molecular and Health Technologies, Bag 10, Clayton MDC, Clayton, VIC 3169, Australia;2. Department of Pharmacology School of Medicine, University of North Carolina Chapel Hill, Chapel Hill, NC 27599, USA |
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| Abstract: | The serendipitous discovery of N-cyclohexyl-8-fluoro-3,3a,4,9b-tetrahydro-1H-thiochromeno4,3-c]isoxazole-1-carboxamide as a selective human serotonin 5-HT2B antagonist with Ki of 42 ± 5 nM is reported herein. A subsequent functional assay indicated little agonist activity compared to 5-HT itself. |
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