2015;231:95-128.
Abstract
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.
KEYWORDS:
2-Arachidonoylglycerol; Anandamide; Cyclooxygenase-2; Drug development; Fatty acid amide hydrolase; Monoacylglycerol lipase; Pain
- PMID:
- 26408159
- [PubMed – as supplied by publisher]
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