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The Potential of Inhibitors of Endocannabinoid Metabolism for Drug Development: A Critical Review
Umeå University, Faculty of Medicine, Department of Pharmacology and Clinical Neuroscience, Pharmacology.
2015 (English)In: Endocannabinoids / [ed] Roger G. Pertwee, Springer International Publishing , 2015, Vol. 231, 95-128 p.Chapter in book (Refereed)
Abstract [en]

The endocannabinoids anandamide and 2-arachidonoylglycerol are metabolised by both hydrolytic enzymes (primarily fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL)) and oxygenating enzymes (e.g. cyclooxygenase-2, COX-2). In the present article, the in vivo data for compounds inhibiting endocannabinoid metabolism have been reviewed, focussing on inflammation and pain. Potential reasons for the failure of an FAAH inhibitor in a clinical trial in patients with osteoarthritic pain are discussed. It is concluded that there is a continued potential for compounds inhibiting endocannabinoid metabolism in terms of drug development, but that it is wise not to be unrealistic in terms of expectations of success.

Place, publisher, year, edition, pages
Springer International Publishing , 2015. Vol. 231, 95-128 p.
, Handbook of Experimental Pharmacology, ISSN 0171-2004 ; 231
Keyword [en]
2-Arachidonoylglycerol; Anandamide; Cyclooxygenase-2; Drug development; Fatty acid amide hydrolase; Monoacylglycerol lipase; Pain
National Category
Pharmacology and Toxicology
URN: urn:nbn:se:umu:diva-120379DOI: 10.1007/978-3-319-20825-1_4PubMedID: 26408159ISBN: 978-3-319-20824-4ISBN: 978-3-319-20825-1OAI: diva2:928645
Available from: 2016-05-16 Created: 2016-05-16 Last updated: 2016-05-30Bibliographically approved

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