Ramosetron HydrochlorideCAS# 132907-72-3 |
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Quality Control & MSDS
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| Cas No. | 132907-72-3 | SDF | Download SDF |
| PubChem ID | 107999 | Appearance | Powder |
| Formula | C17H18ClN3O | M.Wt | 315.8 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 32 mg/mL (101.33 mM; Need ultrasonic and warming) | ||
| Chemical Name | (1-methylindol-3-yl)-[(5R)-4,5,6,7-tetrahydro-3H-benzimidazol-5-yl]methanone;hydrochloride | ||
| SMILES | CN1C=C(C2=CC=CC=C21)C(=O)C3CCC4=C(C3)NC=N4.Cl | ||
| Standard InChIKey | XIXYTCLDXQRHJO-RFVHGSKJSA-N | ||
| Standard InChI | InChI=1S/C17H17N3O.ClH/c1-20-9-13(12-4-2-3-5-16(12)20)17(21)11-6-7-14-15(8-11)19-10-18-14;/h2-5,9-11H,6-8H2,1H3,(H,18,19);1H/t11-;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Ramosetron Hydrochloride Dilution Calculator
Ramosetron Hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1666 mL | 15.8328 mL | 31.6656 mL | 63.3312 mL | 79.164 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL | 12.6662 mL | 15.8328 mL |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 mL | 6.3331 mL | 7.9164 mL |
| 50 mM | 0.0633 mL | 0.3167 mL | 0.6333 mL | 1.2666 mL | 1.5833 mL |
| 100 mM | 0.0317 mL | 0.1583 mL | 0.3167 mL | 0.6333 mL | 0.7916 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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[Analysis of 5-HT3 receptor antagonist, ramosetron hydrochloride, based on receptor occupancy considering its active metabolite].[Pubmed:11725547]
Yakugaku Zasshi. 2001 Nov;121(11):793-8.
Severe nausea and vomiting induced by antineoplastics diminish the patient's quality of life and the ability to tolerate further chemotherapy. Ramosetron Hydrochloride is a 5-HT3 receptor antagonist, which has an active metabolite (M-1), expected to be useful in the inhibition of chemotherapy-induced nausea and vomiting. In the present study, in order to analyze the pharmacological effect of Ramosetron Hydrochloride in a comprehensive manner, we estimated the 5-HT3 receptor occupancy after intravenous administration of Ramosetron Hydrochloride using pharmacokinetic parameters and the dissociation constants for the 5-HT3 receptor. The average total receptor occupancy after intravenous administration of 0.3 mg of Ramosetron Hydrochloride to human was calculated to be 82.9% (ramosetron, 77.8%; M-1, 5.1%), thus exhibiting a significant antiemetic activity. Furthermore, the estimated time course of 5-HT3 receptor occupancies after intravenous administration of 0.3 mg of Ramosetron Hydrochloride suggested a substantial impact of the active metabolite (M-1). It suggested that M-1 contributed to the long duration of binding on the 5-HT3 receptor. The present analysis method should be useful for designing the rational dosage regimen of Ramosetron Hydrochloride and predicting the duration of its antiemetic activity in a quantitative manner.
Mucoadhesive suppositories of ramosetron hydrochloride utilizing Carbopol.[Pubmed:10606783]
Int J Pharm. 2000 Jan 5;193(2):205-12.
Suppositories are the preferable dosage form for patients at home or experiencing nausea. Serotonin (5-HT(3))-receptor antagonists are used to treat vomiting in intravenous or oral administration but not suppository form. Ramosetron Hydrochloride (RAM) is a new 5-HT(3) antagonist which effectively inhibits vomiting, and we prepared RAM suppositories using Witepsol((R)) H-15 (H-15) containing Carbopol((R)) 934P (CP). The viscosity of suppository base and RAM release properties from suppositories were examined. Plasma RAM concentrations after administration of suppositories to rabbits were estimated and irritation of rectal tissues were observed. Antiemetic effects of suppositories were studied using ferrets. The base viscosity increased with addition of CP. Suppositories containing CP exhibited better absorption in rabbits compared to H-15 suppositories, correlated with release behavior. Suppositories containing 2% CP had 2.5 times larger AUC(0-24 h) than H-15 suppositories, and the MRT was prolonged by 5.8 h compared with i.v. administration. 10% CP suppositories administered to rabbits for 5 days did not irritate the tissues. Antiemetic studies indicated that 2% CP suppository of RAM might have the same effect as i.v. administration. These results suggest that RAM suppositories containing CP are safe and useful in once-a-day dosage form for treatment of chemotherapy-induced nausea.
Ramosetron hydrochloride for the prevention of cancer chemotherapy induced nausea and vomiting: The Indian experience.[Pubmed:24818110]
South Asian J Cancer. 2014 Apr;3(2):132-7.
BACKGROUND: Despite the advent of 5-HT3 antagonists, control of delayed gastrointestinal adverse events with cancer chemotherapy is still not optimal. This open label, active controlled, multicentric clinical trial was undertaken to assess the comparative efficacy and safety of ramosetron with ondansetron for the prevention of acute and delayed nausea and vomiting associated with emetogenic cancer chemotherapy in adult patients in India. MATERIALS AND METHODS: Enrolled patients received treatment with Ramosetron Hydrochloride 0.1 mg or ondansetron hydrochloride 4 mg tablets once daily in the morning for 5 days starting 1 h before the start of chemotherapy. Severity grades of nausea and vomiting were recorded on a daily basis for a period of 5 days and complete response rate (CRR) and effective rate (ER) were calculated. Clinical adverse events were recorded and hematological and biochemical investigations were performed for safety assessment. RESULTS: A total of 114 patients in ramosetron group and 100 patients in ondansetron group completed the study and were eligible for efficacy and safety analysis. CRR and ERs show that while ramosetron is non-inferior to ondansetron in the control of early nausea and vomiting (occurring during the first 24 h) after the treatment with emetogenic chemotherapy, it is superior to ondansetron in the control of delayed nausea and vomiting (occurring after the first 24 h). The proportion of patients achieving a cumulative complete response (for the entire study period) is significantly greater in ramosetron group as compared to ondansetron group (27.2% vs. 7.0%; P < 0.001). Ramosetron was well tolerated by all the study participants. CONCLUSIONS: Ramosetron is significantly more effective than ondansetron for the control of delayed nausea and vomiting induced by emetogenic cancer chemotherapy.
