This study showed that lipoxin A4 is an endogenous allosteric enhancer of cannabioid receptor 1 (CB1). Lipoxin A4 increased the affinity of the endogenous cannabinoid anandamide for CB1, and reduction of lipoxin A4 levels in mice reduced the cataleptic effect of anandamide, showing that lipoxin A4 modulates endocannabinoid signalling. Moreover, lipoxin A4 had CB1-mediated neuroprotective effects against amyloid-β (Aβ1–40)-induced memory defects, suggesting that this allosteric modulator could be therapeutically exploited.
ORIGINAL RESEARCH PAPER
Pamplona, F. A. et al. Anti-inflammatory lipoxin A4 is an endogenous allosteric enhancer of CB1 cannabinoid receptor. Proc. Natl Acad. Sci. USA 12 Nov 2012 (doi:10.1073/pnas.1202906109)
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Harrison, C. An endogenous allosteric cannabinoid modulator. Nat Rev Drug Discov 12, 24 (2013). https://doi.org/10.1038/nrd3932
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DOI: https://doi.org/10.1038/nrd3932
