Rimonabant

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Description

Rimonabant is the first selective and orally active antagonist of the central brain cannabinoid receptor (CB1) with IC50 with 13.6 nM and EC50 with 17.3 nM in hCB1 transfected HEK 293 membrane .Rimonabant has been used to afford weight reduction and improvements in cardiometabolic risk factors, however is withdrawn in 2009 due to the severe depressive disorder and anxiety.Besides CB1 inhibition ability, Rimonabant is a dual inhibitor of acyl CoA:cholesterol acyltransferases 1 and 2 . Moreover, Rimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer . Meanwhile, Rimonabant inhibits platelet activation and reduces pro-inflammatory chemokines and leukocytes in Zucker rats .

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