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Rimonabant Oral Anabolic Steroids Anorectic Antiobesity Drug CAS 168273-06-1

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Rimonabant Oral Anabolic Steroids Anorectic Antiobesity Drug CAS 168273-06-1

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Large Image :  Rimonabant Oral Anabolic Steroids Anorectic Antiobesity Drug CAS 168273-06-1

Product Details:
Place of Origin: China
Brand Name: ChineseHormone
Certification: GMP, ISO 9001, USP
Model Number: CAS 168273-06-1
Payment & Shipping Terms:
Minimum Order Quantity: Free samples Available
Price: negotiated
Packaging Details: as your required
Delivery Time: 3-7 working days
Payment Terms: Western Union, MoneyGram, T/T, Bitcoin
Supply Ability: 500-1000 kg / month
Detailed Product Description
MW: 463.787 MF: C22H21Cl3N4O
Appearance: White Crystalline Powder Water Solubility: 0.002 Mg/mL
Alias: SR141716, Acomplia, Zimulti Shipment:: FedEx, TNT, EMS, DHL.UPS,EUB
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Rimonabant Oral Anabolic Steroids Anorectic Antiobesity Drug CAS 168273-06-1

 

CAS number168273-06-1

WeightAverage: 463.787
Monoisotopic: 462.078094435

Chemical Formula :C22H21Cl3N4O

 

Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug that has been withdrawn from the market due to potentially serious side effects. It 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.

 

Uses/potential uses

 

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)."

 

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".

 

Addiction behaviors

 

Rimonabant reduced resumption of cocaine-seeking responses triggered by two of the three most common triggers of relapse in humans: priming and cues. It may also reduce ethanol and opiate-seeking behavior.

 

Short-term memory

 

Tetrahydrocannabinol (THC) is known to impair short-term memory. It was therefore hypothesised that rimonabant may reduce or inhibit the atrophic effects of cannabinoids. Indeed, in animal studies, it significantly improved the ability of rats to encode information into short-term memory.

 

Blockage of cannabis effects

 

Rimonabant blocks the psychoactive and some of the cardiovascular effects of Δ9-tetrahydrocannabinol (THC) in humans without affecting the pharmacokinetics. Rimonabant has been described colloquially as "reverse marijuana", having a depressing effect on appetite inverse to the increased appetite created by cannabinoids.

 

Predicted Properties

 

Property Value Source
Water Solubility 0.002 mg/mL ALOGPS
logP 5.47 ALOGPS
logP 5.91 ChemAxon
logS -5.4 ALOGPS
pKa (Strongest Acidic) 12.42 ChemAxon
pKa (Strongest Basic) 1.68 ChemAxon
Physiological Charge 0 ChemAxon
Hydrogen Acceptor Count 3 ChemAxon
Hydrogen Donor Count 1 ChemAxon
Polar Surface Area 50.16 Å2 ChemAxon
Rotatable Bond Count 4 ChemAxon
Refractivity 122.83 m3·mol-1 ChemAxon
Polarizability 47.96 Å3 ChemAxon
Number of Rings 4 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five Yes ChemAxon
Ghose Filter Yes ChemAxon
Veber's Rule Yes ChemAxon
MDDR-like Rule Yes ChemAxon

 

 

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