Rimonabant in rats with a metabolic syndrome: good news after the depression.
The synthetic cannabinoid CB1 receptor antagonist rimonabant (sold in the United Kingdom under the brand name Acomplia) was reported to improve the profile of cardiovascular risk factors in obese patients with the metabolic syndrome, a cluster of metabolic disorders that often precedes the onset of type II diabetes. Rimonabant is shown in the current issue of British Journal of Pharmacology to attenuate weight gain in Zucker rats, an experimental model of insulin resistance. Neutrophil and monocyte counts were lowered by rimonabant administration. Both platelet activation (by ADP) and aggregation (in response to thrombin) were inhibited. Circulating pro-inflammatory cytokine levels (monocyte chemotactic protein 1, MCP1 and Regulated upon Activation, Normal T-cell Expressed and Secreted, RANTES) were also reduced. Furthermore, fibrinogen levels returned to normal. These favourable anti-inflammatory and anti-thrombotic actions imply for rimonabant a peripheral, direct action on some cardiovascular risk factors.
Di Marzo
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Endocannabinoid Research Group, Institute of Biomolecular Chemistry, C.N.R., Pozzuoli (NA), Italy.
Szallasi
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D000818:Animals; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects; D003863:Depression / Q000139:chemically induced*; D004195:Disease Models, Animal; D018836:Inflammation Mediators / Q000097:blood; D007962:Leukocytes / Q000187:drug effects; D024821:Metabolic Syndrome / Q000097:blood / Q000188:drug therapy* / Q000276:immunology; D010880:Piperidines / Q000009:adverse effects / Q000494:pharmacology*; D015539:Platelet Activation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000009:adverse effects / Q000494:pharmacology*; D011720:Pyrazoles / Q000009:adverse effects / Q000494:pharmacology*; D051381:Rats; D011924:Rats, Zucker; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors; D000077285:Rimonabant
D000893:Anti-Inflammatory Agents; D018836:Inflammation Mediators; D010880:Piperidines; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D000077285:Rimonabant