I am still not sure what to make of Rimonobant, a cannabinoid antagonist designed to help quit smoking and lose weight. I tried the drug a few days and found the effect on appetite to be quite noticable, while at the same time I felt a sense of malaise, which would make sense. Endocannibinoids (drugs our body produces similar to THC in Marijuana) are responsible for regulating a number of things including a sense of well-being and pain management. Think of cannabinoids like opiods, they make you feel good. Block them and you get a good suppression of your appetite (The opposite of the “munchies” effect from Pot) but you also decrease a sense of well-being. Some people have even gone as far as to say it caused them to sink into depression.
The bottom line is that the cannabinoid receptor antagonist Rimonobant has a few very positive effects on fat loss. It decreases food intake and it increases the release of fat in order to be burned for energy. If you can tolerate the side-effects (and quite a few people can) then it’s certainly worth a look into. It helps weight loss, fat loss, and blood sugar control as well as high triglycerides (fat in your blood).
Eur J Pharmacol. 2010 Aug 18. [Epub ahead of print]
Effect of the cannabinoid receptor-1 antagonist rimonabant on lipolysis in rats.
Diabetes & Obesity Pharmacology, Novo Nordisk A/S, Denmark; Department of Pharmacology & Pharmacotherapy, Faculty of Pharmaceutical Sciences, University of Copenhagen, Denmark.
The cannabinoid receptor 1 antagonist, rimonabant, reduces food intake and body weight, but contradictory findings have been reported as to whether the weight-reducing effect is fully accounted for by the reduced food intake or if rimonabant also mediates a lipolytic effect. In the present study, the effect on weight loss was studied in diet-induced obese rats after 3days and 3weeks of exposure to rimonabant, respectively. Induction of lipolysis was examined following acute administration and following 3weeks of repeated dosing. Rimonabant-treated rats lost significantly more weight than their food-restricted controls. This effect was most pronounced in the beginning of the treatment period. No increase in lipolytic activity was found after 3weeks of repeated dosing as measured by microdialysis in adipose tissue whereas acute administration of 10mg/kg produced a significant increase in microdialysate levels of glycerol illustrating an acute stimulation of lipolysis. No equivalent increase in glycerol was, however, observed in vitro following incubation of isolated rat adipocytes with rimonabant. This finding excludes a direct lipolytic action of rimonabant on tissue level. Instead, administration of 10mg/kg produced a significant increase in noradrenaline excretion in diet-induced obese rats, suggesting an increase in sympathoadrenal activity. In conclusion, the present study suggests an acute lipolytic effect of rimonabant mediated through activation of the sympathoadrenal system.
PMID: 20727879 [PubMed - as supplied by publisher]