title: N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
abstract: 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-HT2B antagonist with Ki of 42+/-5 nM is reported herein. A subsequent functional assay indicated little agonist activity compared to 5-HT itself.
authors.affiliation: CSIRO Molecular and Health Technologies, Bag 10, Clayton MDC, Clayton, VIC 3169, Australia.
authors.forename: Yoon Jin
authors.initials: YJ
authors.lastname: Kwon
authors.forename: Simon
authors.initials: S
authors.lastname: Saubern
authors.forename: James M
authors.initials: JM
authors.lastname: Macdonald
authors.forename: Xi-Ping
authors.initials: XP
authors.lastname: Huang
authors.forename: Vincent
authors.initials: V
authors.lastname: Setola
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
mesh_terms: D006575:Heterocyclic Compounds, 3-Ring / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism*; D058830:Serotonin 5-HT2 Receptor Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D006575:Heterocyclic Compounds, 3-Ring; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists