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Description: Rimonabant (also known as SR141716, SR 141716A; A 281) is a novel, potent and selective antagonist (inverse agonist) of cannabinoid CB1 receptor with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is used as an anorectic anti-obesity drug. Its main effect is the reduction of appetite. Rimonabant has shown a 285–fold CB1 selectivity (Ki=1.8nM CB1, 514nM CB2). The affinity of Rimonabant for CB1-Rs is 50-fold higher than for CB2-Rs with a Ki value of 6.18nM for CB1-Rs. In addition, Rimonabant has been revealed to produce changes in ingestive behaviors when treatment alone.
References: FEBS Lett. 1994 Aug 22; 350(2-3):240-4; Int J Cancer. 2009 Sep 1; 125(5):996-1003.
Related CAS#:158681-13-1 (HCl); 168273-06-1 (free base)
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