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 Ki values < 10 nM) and good selectivity for the 5-HT2B receptor vs. other 5-HT2 receptors. Functional assays revealed that the compounds are 5-HT2B