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

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5488-90. doi: 10.1016/j.bmcl.2010.07.074. Epub 2010 Jul 21.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Heterocyclic Compounds, 3-Ring / chemistry*
  • Heterocyclic Compounds, 3-Ring / pharmacology*
  • Humans
  • Receptor, Serotonin, 5-HT2B / metabolism*
  • Serotonin 5-HT2 Receptor Antagonists / chemistry*
  • Serotonin 5-HT2 Receptor Antagonists / pharmacology*
  • Structure-Activity Relationship

Substances

  • Heterocyclic Compounds, 3-Ring
  • Receptor, Serotonin, 5-HT2B
  • Serotonin 5-HT2 Receptor Antagonists