| Size | Price | Stock | Qty |
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| 100mg |
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| Other Sizes |
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Dolasetron mesylate hydrate (MDL-73147EF hydrate; MDL-73147) is a potent serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Little information is available on the use of dolasetron during breastfeeding. Until more data become available, dolasetron should be used with caution during breastfeeding. An alternate drug may be preferred. ◉ Effects in Breastfed Infants A double-blind study randomized 160 women receiving an elective cesarean section under spinal anesthesia to receive either sufentanil for patient-controlled intravenous analgesia (standard care) or standard care plus dexmedetomidine. Dexmedetomidine was given as 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg per hour until the end of surgery. Patient in this latter group received dexmedetomidine plus sufentanil for patient-controlled intravenous analgesia postoperatively for 2 days. Both groups had 25 mg of dolasetron added to the patient-controlled intravenous analgesia solution and all mothers breastfed their infants. Both groups had good neonatal behavioral neurological assessments on days 1 and 2 postpartum.[1] ◉ Effects on Lactation and Breastmilk A double-blind study randomized 160 women receiving an elective cesarean section under spinal anesthesia to receive either sufentanil for patient-controlled intravenous analgesia (standard care) or standard care plus dexmedetomidine. Dexmedetomidine was given as 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg per hour until the end of surgery. Patient in this latter group received dexmedetomidine plus sufentanil for patient-controlled intravenous analgesia postoperatively for 2 days. Both groups had 25 mg of dolasetron added to the patient-controlled intravenous analgesia solution. Patients who received dexmedetomidine had a shorter time to the first lactation (28 vs 34 hours), achieved exclusive breastfeeding sooner (8 vs 11 days) and had a greater amount of milk on the second day postpartum.[1] |
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| References |
[3]. Long-term Use of Ondansetron, Dolasetron and Granisetron for the Prevention of Nausea and Vomiting: A Review of the Clinical Effectiveness and Safety [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2014 Apr 23. Available from http://www.ncbi.nlm.nih.gov/books/NBK269203/ PubMed PMID: 25610941. |
| Additional Infomation |
Dolasetron Mesylate is an indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, dolasetron mesylate competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. (NCI04)
See also: Dolasetron Mesylate (annotation moved to). |
| Molecular Formula |
C20H26N2O7S
|
|---|---|
| Molecular Weight |
438.4946
|
| Exact Mass |
438.146
|
| CAS # |
878143-33-0
|
| Related CAS # |
Dolasetron;115956-12-2;Dolasetron Mesylate;115956-13-3
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| PubChem CID |
6918119
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| Appearance |
White to off-white solid powder
|
| Melting Point |
178 °C
|
| LogP |
2.634
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
30
|
| Complexity |
627
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CS(=O)(=O)O.C1[C@@H]2CC(C[C@H]3N2CC(=O)C1C3)OC(=O)C4=CNC5=CC=CC=C54.O
|
| InChi Key |
QTFFGPOXNNGTGZ-RCSCTSIBSA-N
|
| InChi Code |
InChI=1S/C19H20N2O3.CH4O3S.H2O/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17;1-5(2,3)4;/h1-4,9,11-14,20H,5-8,10H2;1H3,(H,2,3,4);1H2/t11?,12-,13+,14?;;
|
| Chemical Name |
methanesulfonic acid;[(3S,7R)-10-oxo-8-azatricyclo[5.3.1.03,8]undecan-5-yl] 1H-indole-3-carboxylate;hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~570.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2806 mL | 11.4028 mL | 22.8055 mL | |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5611 mL | |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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