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Issue 10, 2012
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Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

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Abstract

Fatty acid amide hydrolase (FAAH) inhibition is a promising target for the treatment of pain, anxiety and depression. The vast majority of FAAH inhibitors contain an electrophilic moiety and are known to react covalently with the enzyme. Herein we present the discovery of potent inhibitors, such as RN-450 29, which are based upon a novel tetrahydropyridopyridine scaffold lacking an obvious electrophilic site, and which appear to inhibit FAAH in a reversible and non-covalent manner.

Graphical abstract: Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

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Publication details

The article was received on 04 Jun 2012, accepted on 19 Jul 2012 and first published on 25 Jul 2012


Article type: Concise Article
DOI: 10.1039/C2MD20146A
Med. Chem. Commun., 2012,3, 1258-1263

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    Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)

    S. Gowlugari, J. DeFalco, M. T. Nguyen, C. Kaub, C. Chi, M. A. J. Duncton, D. E. Emerling, M. G. Kelly, J. Kincaid and F. Vincent, Med. Chem. Commun., 2012, 3, 1258
    DOI: 10.1039/C2MD20146A

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