Referenced in: none

Automatically associated channels: Kv11.1

Title: Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.

Authors: Kensuke Kobayashi, Tetsuya Kato, Izumi Yamamoto, Atsushi Shimizu, Sayaka Mizutani, Masanori Asai, Hiroshi Kawamoto, Satoru Ito, Takashi Yoshizumi, Mioko Hirayama, Satoshi Ozaki, Hisashi Ohta, Osamu Okamoto

Journal, date & volume: Bioorg. Med. Chem. Lett., 2009 Jun 1 , 19, 3100-3

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/19398200

Abstract
A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over binding affinity for hERG and other opioid receptors.