Issue 4, 2015

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-HT2Bantagonists.

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

Associated articles

Supplementary files

Article information

Article type
Concise Article
Submitted
18 Sep 2014
Accepted
15 Dec 2014
First published
15 Dec 2014

Med. Chem. Commun., 2015,6, 601-605

Author version available

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

S. Ponnala, N. Kapadia and W. W. Harding, Med. Chem. Commun., 2015, 6, 601 DOI: 10.1039/C4MD00418C

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