N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
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.
Kwon
Yoon Jin
YJ
CSIRO Molecular and Health Technologies, Bag 10, Clayton MDC, Clayton, VIC 3169, Australia.
Saubern
Simon
S
Macdonald
James M
JM
Huang
Xi-Ping
XP
Setola
Vincent
V
Roth
Bryan L
BL
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
D006575:Heterocyclic Compounds, 3-Ring; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists