Referenced in: none

Automatically associated channels: Kv11.1

Title: Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.

Authors: Kensuke Kobayashi, Minaho Uchiyama, Hirokatsu Ito, Hirobumi Takahashi, Takashi Yoshizumi, Hiroki Sakoh, Yasushi Nagatomi, Masanori Asai, Hiroshi Miyazoe, Tomohiro Tsujita, Mioko Hirayama, Satoshi Ozaki, Takeshi Tani, Yasuyuki Ishii, Hisashi Ohta, Osamu Okamoto

Journal, date & volume: Bioorg. Med. Chem. Lett., 2009 Jul 1 , 19, 3627-31

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/19447610

Abstract
The synthesis and biological evaluation of new potent opioid receptor-like 1 antagonists are presented. A structure-activity relationship (SAR) study of arylpyrazole lead compound 1 obtained from library screening identified compound 31, (1S,3R)-N-{[1-(3-chloropyridin-2-yl)-5-(5-fluoro-6-methylpyridin-3-yl)-4-methyl-1H-pyrazol-3-yl]methyl}-3-fluorocyclopentanamine, which exhibits high intrinsic potency and selectivity against other opioid receptors and hERG potassium channel.