Identification of tris-(phenylalkyl)amines as new selective h5-HT2B receptor antagonists

Abstract

A series of tris-(phenylalkyl)amines was synthesized and evaluated for affinity to human 5-HT₂ receptors. In general, the compounds displayed high affinity (4 of 11 analogs had K_i values < 10 nM) and good selectivity for the 5-HT_2B receptor vs. other 5-HT₂ receptors. Functional assays revealed that the compounds are 5-HT_2Bantagonists.