ACOMPLIA
Rimonabant
CAS: 168273-06-1
Molecular Formula: C22H21Cl3N4O
ACOMPLIA - Names and Identifiers
| Name | Rimonabant |
| Synonyms | A 281 xibuqum ACOMPLIA Rimonabant RIMONABANT RIMONABANT(ACOMPLIA,SR141716) 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidinopyrazole-3-carboxamide 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-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-(piperidin-1-yl)-1H-pyrazole-3-carboxamide |
| CAS | 168273-06-1 |
| EINECS | 200-223-5 |
| InChI | InChI=1/C22H21Cl3N4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
ACOMPLIA - Physico-chemical Properties
| Molecular Formula | C22H21Cl3N4O |
| Molar Mass | 463.79 |
| Density | 1.41±0.1 g/cm3(Predicted) |
| Melting Point | 154.7 °C |
| Boling Point | 627.6℃ at 760 mmHg |
| Solubility | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 20 mg/ml). |
| Appearance | White or nearly white crystalline powder |
| Color | White |
| pKa | 11.31±0.20(Predicted) |
| Storage Condition | RT |
| Stability | Stable for 1 year from date of purchase as supplied. Protect from moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.668 |
| Use | An immunomodulatory CB1 receptor inverse agonist. |
ACOMPLIA - Introduction
Rimonabant is a brain center cannabinoid receptor (CB1) specific oral antagonist. IC50 concentration was 13.6 nM and EC50 concentration was 17.3 nM in hCB1 transfected HEK293 cells.
Last Update：2022-10-16 17:14:20
ACOMPLIA - Reference Information
| Introduction | Rimonabant hydrozolide is a cannabinoid receptor 1(CB1) antagonist, by blocking cannabinoid receptors in brain tissue to reduce appetite and tobacco addiction, it can be used to treat obesity, tobacco addiction, hypertension, dyslipidemia, type 2 diabetes and metabolic syndrome, while lowering cholesterol, it has the effect of preventing heart disease and diabetes in obese people, and has been listed in several countries in 2006. In addition, basic and clinical studies have confirmed that rimonabant can effectively improve obesity associated with hyperglycemia, insulin resistance and lipid metabolism disorders. |
| trait | white powder |
| properties | off-white to white crystalline powder, easily soluble in methanol. Melting Point: 230 ℃ ~ 240 ℃ weight loss on drying: ≤ 0.5% PH:(10% aqueous solution) 4-7 heavy metals: ≤ 10ppm TLC: only one spot content: ≥ 99.5% indications: new weight loss, smoking cessation, hypolipidemic, medical raw materials. |
| pharmacological action | as a specific CB1 antagonist, rimonabant achieves its anti-obesity effect by acting on both central and peripheral CB1 receptors, respectively. The weight loss effect of rimonabant can be divided into two stages: in the initial stage of drug treatment, the weight loss results from the obvious appetite suppression and the decrease of food intake caused by the drug antagonizing the central part of CB1 receptor. After that, the body's tolerance to the drug is produced, and the appetite suppression effect is weakened or even disappeared. The subsequent long-term weight-loss effect arises from the peripheral mechanism of action of the drug, I .e., rimonabant regulates energy metabolism in the body by acting on CB1 receptors on the gastrointestinal tract, adipocytes, skeletal muscle and liver, thereby reducing body weight. |
| Application | Rimonabant hydrozolide is a cannabinoid receptor (CB1) antagonist, by blocking cannabinoid receptors in brain tissue to reduce appetite and tobacco addiction, it can be used to treat obesity, tobacco addiction, hypertension, dyslipidemia, type 2 diabetes and metabolic syndrome, while lowering cholesterol, it has the effect of preventing heart disease and diabetes in obese people, and has been listed in several countries in 2006. In addition, basic and clinical studies have confirmed that rimonabant can effectively improve the hyperglycemia, insulin resistance and lipid metabolism disorder associated with obesity. However, at present, the understanding of the above mechanism of rimonabant is still superficial, and the more exact mechanism still needs further study and clarification. In view of its obvious economic benefits and social value, the development of the synthesis process of rimonabant hydrochloride with industrial potential has a broad market prospect. |
| Use | new weight loss drug, and can be applied to smoking cessation. rimonabant is a new weight loss drug and can be used to stop smoking. Rimonabant, a new weight-loss drug, can not only lose weight, but also lower blood pressure, cholesterol and blood sugar. More than a year of clinical research in China found that subjects took it for one to two months, the average weight can be reduced by six to eight kilograms. |
| weight loss drug | rimonabant is a weight loss drug developed by the French company Sanofi-Aventis, also the first cannabinoid type 1 receptor (CB1) antagonist to be used in the treatment of obesity, acts by selectively blocking the cannabinoid-1(cannabinoid-1,CB1) receptor in the EC system, can significantly reduce weight, shrink waist circumference, reduce cardiovascular disease and other risk factors, but also can improve blood lipids and insulin resistance and metabolic syndrome, especially for the presence of clinical obesity or heart disease risk. |
| adverse reactions | although the effect of rimonabant in the treatment of weight loss is significant, the adverse reactions reported in recent years can not be ignored. In RIO-Europe, people taking rimonabant at doses of 5mg and 20mg were more frequent than placebo controls Nausea Vomit (5.1%,12.9% and 4.3%), Diarrhea (6.0%,7.2% and 3.0%, respectively), dizziness (7.0%,8.7% and 4.9%, respectively), confusion (2.3%,3.7% and, respectively). These phenomena also appeared in RIO-Lipids of the studies. A combined analysis of four randomized controlled studies showed that rimonabant was associated with an increase in psychiatric serious adverse events, namely depression and Anxiety. |
Last Update：2024-04-09 21:01:54
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