Fenofibrate May Mimic Cannabinoid Receptor Stimulation

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Fenofibrate May Mimic Cannabinoid Receptor Stimulation
Fenofibrate May Mimic Cannabinoid Receptor Stimulation

Researchers have discovered that a common medication indicated for the treatment of high cholesterol may stimulate the same peroxisome proliferator-activated receptors (PPARs) as cannabinoids, which could lead to a new class of cannabis-like drugs to treat a range of conditions.

In this study appearing the The FASEB Journal, Richard S. Priestley, PhD, of the University of Nottingham Medical School, and colleagues cultured cells containing human recombinant cannabinoid type 1 (CB1) or cannabinoid type 2 (CB2) receptors; the cells were then exposed to a tracer compound that binds to cannabinoid receptors. Fenofibrate was not only able to displace the tracer (suggesting a similar binding to the receptors), but acted as an agonist at the CB2 receptor and a partial agonist at the CB1 receptor with a decrease in functional response at higher concentrations.

These results suggest that some of the effects of fenofibrate may be controlled by cannabinoid receptors, despite the previous belief that fenofibrate's mechanism of action was the active moiety of fenofibric acid. The cannabinoid receptors in this study may be a future target for drugs indicated for treating pain, appetite stimulation, nausea, and immune and various psychiatric and neurological conditions.

Fenofibrate is currently indicated as adjunct to diet in hypertriglyceridemia and to reduce elevated LDL cholesterol, total cholesterol, triglycerides and apolipoprotein-B, and to increase HDL cholesterol, in primary hyperlipidemia and mixed dyslipidemia.

Reference

  1. Priestley RS et al. FASEB J. 2015;29(4):1446-1455.
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