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CAS NO.168273-06-1
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Product Name: Rimonabant
Product Details:
Product Name | Rimonabant |
Synonyms | Acomplia;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 |
CAS | 168273-06-1 |
EINECS | N/A |
MF | C22H21Cl3N4O |
MW | 463.79 |
Molecular Structure | |
Standard | Enterprise Standard |
Assay | 98% |
Chemical Properties | White to off white powder |
Usage | Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. |
Description:
Rimonabant is one of the most recent drugs created for the treatment of obesity. This drug acts as a blockade for endocannabinoid receptors found in the brain and peripheral organs that play an important role on carbohydrate and fat metabolism. Clinical studies have confirmed that, when used in combination with a low calorie diet, rimonabant promotes loss in body weight, loss in abdominal circumference, and improvements in dyslipidemia.
Rimonabant is also being tested as a potential anti-smoking treatment since endocannabinoids are related to the pleasurable effect of nicotine. Thus, rimonabant constitutes a new therapeutic approach to obesity and cardiovascular risk factors. Studies show effectiveness in weight loss; however, side effects such as psychiatric alterations have been reported, including depression and anxiety. These side effects have led the FDA (Food and Drug Administration) to not approve this drug in the United States. For a more complete evaluation on the safety of this drug, additional studies are in progress. Rimonabant (trade name Acomplia) is an anorectic antiobesity drug that has been withdrawn from the market due to potentially serious side effects. Rimonabant was approved for use in Europe and other countries, but never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor CB1.It has also been shown to be a μ-opioid receptor antagonist (possibly the contributing factor in its reported dysphoric qualities).Its main effect is reduction in appetite. The Rimonabant is a very great weight loss powders in nowadays markets ,and its purity is very high ,the contents is for 99% ;especially for smoker and is also for patients with cardiovascular diseases. Rimonabant is from the class of medicines called cannabinoid receptor antagonists. This drug makes it possible for you to handle dieting easier allowing you to lose excessive weight if you have been diagnosed with obesity. This medicine works by selectively blocking certain receptors in the brain and other organs that control metabolism, including liver, gastrointestinal tract and adipose tissue. In addition to the beneficial effects of reducing food cravings this drug has demonstrated to increase the levels of good cholesterol (HDL) and decrease the levels of bad cholesterol (triglycerides). According to the clinical studies of this medicine about a third of people who took rimonabant lost 10% of their body weight in the first two years of the treatment, and what's even more important - were able to maintain the result during this time
Rimonabant (Acomplia) is an efficient cannabinoid receptor antagonist that lowers your food yearnings and therefore helps you to burn fat without excessive emotional stress. It does not work on its own, in lieu of in combination with diet programs and regular exercising. 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.
Application:
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.
1) 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 kg vs -1.6 [0.2] kg; P<.001), waist circumference (-6.1 [0.2] cm vs -2.5 ] cm; P<.001), and level of triglycerides (percentage change, -5.3 vs 7.9 ; P<.001) and a greater increase in level of high-density lipoprotein cholesterol (percentage change, 12.6 vs 5.4 ; P<.001)."
2) 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.
COA:
Product Name
|
Rimonabant | ||
Test Items
|
Specification | Test Results | |
Appearance
|
Off white crystalline powder | Off white crystalline powder | |
Melting Point
|
230℃~240℃ | 233.2℃~236.1℃ | |
L.O.D
|
≤0.5% | 0.23% | |
Solubility
|
Freely soluble in methanol | Conforms | |
Heavy metals(Pb)
|
≤10ppm | 10ppm | |
Assay
|
≥99.5% | 99.65% |
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