Referenced in: none

Automatically associated channels: Kv11.1

Title: Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.

Authors: Wu Yang, Yufeng Wang, Jacques Y Roberge, Zhengping Ma, Yalei Liu, R Michael Lawrence, David P Rotella, Ramakrishna Seethala, Jean H M Feyen, John K Dickson

Journal, date & volume: Bioorg. Med. Chem. Lett., 2005 Feb 15 , 15, 1225-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/15686947

Abstract
A structure-activity relationship study of the amine portion of the calcilytic compound NPS-2143 resulted in the discovery of substituted 2-benzylpyrrolidines as replacements for the 1,1-dimethyl-2-naphthalen-2-yl-ethylamine. When compared to NPS-2143, a newly discovered compound, 3h, exhibited similar potency as a calcium-sensing receptor (CaR) antagonist and a superior human ether-a-go-go related gene (hERG) profile.