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An update on PPAR activation by cannabinoids
Abstract
Some cannabinoids activate the different isoforms of PPARs (α, β and γ), as shown through the use of reporter gene assays, binding studies, selective antagonists and knockout studies. Activation of all isoforms, but primarily PPARα and γ, mediates some (but not all) of the analgesic, neuroprotective, neuronal function modulation, anti‐inflammatory, metabolic, anti‐tumour, gastrointestinal and cardiovascular effects of some cannabinoids, often in conjunction with activation of the more traditional target sites of action such as the cannabinoid CB 1 and CB 2 receptors and the TRPV1 ion channel. PPARs also mediate some of the effects of inhibitors of endocannabinoid degradation or transport. Cannabinoids may be chaperoned to the PPARs by fatty acid binding proteins. The aims of this review are to update the evidence supporting PPAR activation by cannabinoids and to review the physiological responses to cannabinoids that are mediated, and not mediated, by PPAR activation.
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eCBs and eCB-like metabolites exert their cellular functions through various molecular mechanisms, including by acting as ligands for transcription factors of the PPAR gene family.
“eCBs and eCB-like metabolites exert their cellular functions through various molecular mechanisms, including by acting as ligands for transcription factors of the PPAR gene family30,31.”
From Interaction of sortilin with apolipoprotein E3 enables neurons to use long-chain fatty acids as alternative metabolic fuel (2025) · cites this paper as [30]
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“On the other hand, inhibition of FABPs reduces inflammatory pain in mice, and this can be inhibited by CB1 receptor or PPARα antagonists (Kaczocha et al., 2014), suggesting here that the FABP-direct degradation of endocannabinoids can also limit their ability to activate PPARα.”
BackgroundInfluentialFat-induced satiety factor oleoylethanolamide enhances memory consolidation
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Metadata
- Authors
- O'Sullivan, S. E.
- Affiliations
- School of Medicine, Royal Derby Hospital University of Nottingham
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2016-05-19
- Volume
- 173
- Issue
- 12
- Pages
- 1899-1910
- ISSN
- 0007-1188
- 1476-5381
- Cited by
- 449
- References
- 11
- Language
- en
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