Identification of MK-1925: A selective,orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist |
| |
Authors: | Kensuke Kobayashi Tomohiro Tsujita Hirokatsu Ito Satoshi Ozaki Takeshi Tani Yasuyuki Ishii Shoki Okuda Kiyoshi Tadano Takahiro Fukuroda Hisashi Ohta Osamu Okamoto |
| |
Affiliation: | Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan |
| |
Abstract: | Structure–activity relationship studies directed toward improving the metabolic stability of compound 1 resulted in the identification of 3-[5-(3,5-difluorophenyl)-3-({[(1S,3R)-3-fluorocyclopentyl]amino}methyl)-4-methyl-1H-pyrazol-1-yl]propanenitrile 39 (MK-1925) as a selective, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. The compound also showed in vivo efficacy after oral dosing. Therefore, compound 39 was selected to undergo further studies as a clinical candidate. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|