Referenced in: none

Automatically associated channels: Kv11.1

Title: Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.

Authors: Su Jin Gu, Jae Kyun Lee, Ae Nim Pae, Hye Jin Chung, Hyewon Rhim, So Yeob Han, Sun-Joon Min, Yong Seo Cho

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 May 1 , 20, 2705-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20382529

Abstract
We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases.