Vnitr Lek 2006, 52(6):615-618

Impact of endocannabinoid system in modulation of the metabolic syndrome

A. Šulcová

Farmakologický ústav Lékařské fakulty MU, Brno, vedoucí prof. MUDr. Alexandra Šulcová, CSc.

Endocannabinoid system, the complex of specific cannabinoid receptors (CB₁ and CB₂ subtypes) and their endogenous agonistic ligands (endocannabinoids) plays, besides others, an important role in the central and peripheral regulation of food intake, fat accumulation, and lipid and glucose metabolism. Alterations of these functions are associated with endocannabinoid system hyperactivity. The cannabinoid receptor CB₁ antagonist rimonabant normalizes the over activated endocannabinoid system which contributes to the regulation of energy homeostasis, and improves lipid and glucose metabolism - decreases body weight, waist circumference, intra-abdominal obesity and triglycerides, increases HDL-C, improves insulin sensitivity according to HOMA index. Results of the international multicentric clinical trials confirm that rimonabant is well tolerated and show antiatherogenic effects (increased adiponectin, decreased marker of inflammation CRP and improvement of LDL profile) as well as decreased percentage of subjects with NCEP/ATPIII (National Cholesterol Education Program Adult Treatment Panel III) defined metabolic syndrome. Thus, the CB₁ cannabinoid receptor antagonist rimonabant is suggested to be a prospective drug decreasing cardiometabolic risk factors.

Keywords: cannabinoid receptors; endocannabinoids; antagonist rimonabant; cardiometabolic risk factors

Received: March 8, 2006; Accepted: April 27, 2006; Published: June 1, 2006  Show citation