Canna~Fangled Abstracts

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.

By January 31, 2014 No Comments
2014 Jan 31. pii: S0960-894X(14)00094-8. doi: 10.1016/j.bmcl.2014.01.064. [Epub ahead of print]

pm81-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

Analgesia, Crystal structure, Endo-cannabinoids, Enzymes, Fatty acid amide hydrolase (FAAH)

PMID:

 

24513048

 

[PubMed – as supplied by publisher]
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