CSIRO Molecular and Health Technologies, Bag 10, Clayton MDC, Clayton, VIC 3169, Australia.
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5488-90. doi: 10.1016/j.bmcl.2010.07.074. Epub 2010 Jul 21.
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.
本文报道了 N-环己基-8-氟-3,3a,4,9b-四氢-1H-噻吩并[4,3-c]异噁唑-1-甲酰胺作为一种选择性人 5-羟色胺 5-HT2B 拮抗剂的偶然发现，其 Ki 值为 42+/-5 nM。随后的功能测定表明，与 5-HT 本身相比，该化合物的激动活性较小。
