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CAS NO.168273-06-1
A(1-10)Metric TonA(20-50)Metric Ton
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CAS:168273-06-1
MF:C22H21Cl3N4O
MW:463.79
Synonyms: ACOMPLIA;RIMONABANT;RIMONABANT(ACOMPLIA,SR141716);5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidinopyrazole-3-carboxamide;1H-Pyrazole-3-carboxamide, 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-;5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide;A 281;Sr 141716
Use:
Rimonabant is a weight loss drug, can significantly reduce weight, reduce waist circumference and reduce risk factors for cardiovascular disease, but also can improve blood lipids and insulin resistance and metabolic syndrome, especially for the presence of clinical obesity or heart disease people at risk.
Rimonabant as a new weight loss drug, can also be used to quit smoking. Not only lose weight, but also lower blood pressure, cholesterol and blood sugar, clinical study found that subjects taking one to two months later, the weight can be reduced on average six to eight kilograms.
Applications
Rimonabant is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States. This decision was made after a U.S. advisory panel recommended the medicine not be approved because it may increase suicidal thinking and depression.
Rimonabant works by blocking endogenous cannabinoid from binding to neuronal CB1 receptors. The activation of these receptors by endogenous cannabinoids, such as anadamide, increases an individuals appetite. By blocking the activation of the receptors, appetite suppression may occur.
Obesity
In a 2006 (2 year) study reported in JAMA, "Compared with the placebo group, the 20 mg of rimonabant group produced greater mean (SEM) reductions in weight (-6.3 [0.2] kg vs -1.6 [0.2] kg; P<.001), waist circumference (-6.1 [0.2] cm vs -2.5 [0.3] cm; P<.001), and level of triglycerides (percentage change, -5.3 [1.2] vs 7.9 [2.0]; P<.001) and a greater increase in level of high-density lipoprotein cholesterol (percentage change, 12.6 [0.5] vs 5.4 [0.7]; P<.001)." [12]
Smoking cessation
Rimonabant may also be found to be effective in assisting some smokers to quit smoking. Sanofi is currently conducting studies to determine the possible value of rimonabant in smoking-cessation therapy. The Studies with Rimonabant and Tobacco Use (STRATUS) program involves more than 6,000 subjects. STRATUS is designed to explore two smoking-related therapies: first, to use rimonabant directly to aid in smoking cessation; second, to help prevent weight gain in former smokers. Initial results apparently suggest rimonabant is effective for both uses. However, the FDA has explicitly stated to Sanofi that, without additional studies, rimonabant cannot be approved in the United States for smoking cessation therapy. According to a Cochrane Collaboration review in 2007, rimonabant "may increase the odds of quitting approximately 11/2-fold".
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