| Literature DB >> 24513048 |
John M Keith1, Natalie Hawryluk2, Richard L Apodaca2, Allison Chambers2, Joan M Pierce2, Mark Seierstad2, James A Palmer2, Michael Webb2, Mark J Karbarz2, Brian P Scott2, Sandy J Wilson2, Lin Luo2, Michelle L Wennerholm2, Leon Chang2, Michele Rizzolio2, Sandra R Chaplan2, J Guy Breitenbucher2.
Abstract
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.Entities:
Keywords: Analgesia; Crystal structure; Endo-cannabinoids; Enzymes; Fatty acid amide hydrolase (FAAH)
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Year: 2014 PMID： 24513048 DOI： 10.1016/j.bmcl.2014.01.064
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823