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CAS: 168273-06-1
分子式: C22H21Cl3N4O. ClH
分子量: 500.25
外観: 白色またはほぼ白色の結晶粉末
純度: ≥ 99% HPLCによる
融点: 272.25 ℃
使用法: 医薬品中間体, 微細有機合成と触媒, ヘルスケア製品など

Rimonabant (Acomplia) was the first in a new class of therapeutic agents called Cannabinoid-1 Receptor Blockers (CB1). Acomplia was studied for use in the treatment of obesity and related conditions.

An experimental wonder drug, Rimonabant, helps you lose weight, quit smoking and it also helps protect your heart. Trials have shown that 33% of people on Rimonabant lost 10% of body weight and kept their weight down for two years - this is a record, no other diet drug has managed to keep a person's weight down for so long. The second 33% lost 5% of body weight and kept it down. As well as keeping you lean, the drug also helps you quit the smoking habit. This will be of great interest for many smokers who are afraid to give up because they say they will put on loads of weight if they do.

Rimonabant 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.

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 (-6.3kg vs -1.6kg; P<.001), waist circumference (-6.1cm vs -2.5cm; P<.001), and level of triglycerides (percentage change, -5.3vs 7.9; P<.001) and a greater increase in level of high-density lipoprotein cholesterol (percentage change, 12.6vs 5.4; P<.001)."

2. 禁煙:
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. しかし, the FDA has explicitly stated to Sanofi that, without additional studies, rimonabant cannot be approved in the United States for smoking cessation therapy.

分析項目 仕様 結果
Assay by (HPLC) 99%-101% 99.43%
外観 White to off White powder 準拠
Odor and taste 無臭 準拠
識別 陽性反応 準拠
Mesh size/sieve analysis 100% 合格 80 メッシュ 準拠
乾燥減量 1% マックス 0.78%
≤2.0% 0.1%
強熱時の残留物 01% マックス 準拠
融点 272.25 ℃ 準拠
Boiling point 627 .69 ℃ 準拠
屈折率 N20O1.67 準拠
PH 50-7.0 6.5
pK Values pK. 11.31(Predicted). pK„ 3. 22 (Predicted) 準拠
溶解性 Soluble in ethanol (-20 mg/ml). DMSO (25 mg/ml) .DMF (-20mg/ml). そして水 (< 1 mg/ml) 準拠
重金属 NMT 10ppm 準拠
Microbiological Control 78cfu/g 78cfu/g
総プレート数 1000 cfu/g Max ネガティブ
Fungi <100/g ネガティブ
サルモネラ ネガティブ ネガティブ
Coll negative negative
結論 資格のある

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