Synonym
Dolasetron; Dolasetronum; Anzemet Cinv; MDL 73147; MDL73147; MDL-73147
IUPAC/Chemical Name
[(3S,7R)-10-oxo-8-azatricyclo[5.3.1.03,8]undecan-5-yl] 1H-indole-3-carboxylate
InChi Key
UKTAZPQNNNJVKR-DBBXXEFVSA-N
InChi Code
InChI=1S/C19H20N2O3/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/h1-4,9,11-14,20H,5-8,10H2/t11?,12-,13?,14?/m1/s1
SMILES Code
C1[C@@H]2CC(C[C@H]3N2CC(=O)C1C3)OC(=O)C4=CNC5=CC=CC=C54
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Dolasetron (MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
25.0 |
77.07 |
| DMSO |
132.3 |
407.97 |
| DMSO:PBS (pH 7.2) (1:1) |
0.5 |
1.54 |
| Ethanol |
16.0 |
49.33 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
324.37
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
TBD
1: 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.
2: Balfour JA, Goa KL. Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery. Drugs. 1997 Aug;54(2):273-98. Review. PubMed PMID: 9257083.
3: Rochford M, Kiernan TJ, Aziz A. Dolasetron overdose resulting in prolonged QTc interval and severe hypotension: a case report and literature review. Emerg Med J. 2007 Jul;24(7):515-7. Review. PubMed PMID: 17582056; PubMed Central PMCID: PMC2658414.
4: Ogilvie GK. Dolasetron: a new option for nausea and vomiting. J Am Anim Hosp Assoc. 2000 Nov-Dec;36(6):481-3. Review. PubMed PMID: 11105883.
5: Hui YF, Ignoffo RJ. Dolasetron. A new 5-hydroxytryptamine3 receptor antagonist. Cancer Pract. 1997 Sep-Oct;5(5):324-8. Review. PubMed PMID: 9341357.
6: Eremita D. Dolasetron for chemo nausea. RN. 2001 Mar;64(3):38-40. Review. PubMed PMID: 11288648.
7: Tricco AC, Soobiah C, Blondal E, Veroniki AA, Khan PA, Vafaei A, Ivory J, Strifler L, Ashoor H, MacDonald H, Reynen E, Robson R, Ho J, Ng C, Antony J, Mrklas K, Hutton B, Hemmelgarn BR, Moher D, Straus SE. Comparative safety of serotonin (5-HT3) receptor antagonists in patients undergoing surgery: a systematic review and network meta-analysis. BMC Med. 2015 Jun 18;13:142. doi: 10.1186/s12916-015-0379-3. Review. PubMed PMID: 26084332; PubMed Central PMCID: PMC4472408.
8: Rojas C, Raje M, Tsukamoto T, Slusher BS. Molecular mechanisms of 5-HT(3) and NK(1) receptor antagonists in prevention of emesis. Eur J Pharmacol. 2014 Jan 5;722:26-37. doi: 10.1016/j.ejphar.2013.08.049. Epub 2013 Oct 31. Review. PubMed PMID: 24184669.
9: Broder MS, Faria C, Powers A, Sunderji J, Cherepanov D. The Impact of 5-HT3RA Use on Cost and Utilization in Patients with Chemotherapy-Induced Nausea and Vomiting: Systematic Review of the Literature. Am Health Drug Benefits. 2014 May;7(3):171-82. Review. PubMed PMID: 24991400; PubMed Central PMCID: PMC4070626.
10: Mori-Vogt S, Blazer M. Palonosetron for the prevention of chemotherapy-induced nausea and vomiting. Expert Rev Anticancer Ther. 2013 Aug;13(8):919-36. doi: 10.1586/14737140.2013.814412. Review. PubMed PMID: 23984894.
11: Fujii Y. Management of postoperative nausea and vomiting in women scheduled for breast cancer surgery. J Anesth. 2011 Dec;25(6):917-22. doi: 10.1007/s00540-011-1241-1. Epub 2011 Oct 1. Review. Retraction in: Hirota K. J Anesth. 2013 Apr;27(2):322. PubMed PMID: 21964679.
12: Rubenstein EB. Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9. Review. PubMed PMID: 16163194.
13: Botrel TE, Clark OA, Clark L, Paladini L, Faleiros E, Pegoretti B. Efficacy of palonosetron (PAL) compared to other serotonin inhibitors (5-HT3R) in preventing chemotherapy-induced nausea and vomiting (CINV) in patients receiving moderately or highly emetogenic (MoHE) treatment: systematic review and meta-analysis. Support Care Cancer. 2011 Jun;19(6):823-32. doi: 10.1007/s00520-010-0908-8. Epub 2010 May 22. Review. PubMed PMID: 20495832.
14: Fujii Y. Current review of ramosetron in the prevention of postoperative nausea and vomiting. Curr Drug Saf. 2011 Apr;6(2):122-7. Review. PubMed PMID: 21382011.
15: Board T, Board R. The role of 5-HT3 receptor antagonists in preventing postoperative nausea and vomiting. AORN J. 2006 Jan;83(1):209-16, 219-20. Review. PubMed PMID: 16528908.
16: Navari RM, Koeller JM. Electrocardiographic and cardiovascular effects of the 5-hydroxytryptamine3 receptor antagonists. Ann Pharmacother. 2003 Sep;37(9):1276-86. Review. PubMed PMID: 12921512.
17: Blower PR. 5-HT3-receptor antagonists and the cytochrome P450 system: clinical implications. Cancer J. 2002 Sep-Oct;8(5):405-14. Review. PubMed PMID: 12416899.
18: Alon E, Biro P. [Prevention and treatment of postoperative nausea and vomiting with 5-HT3-receptor blockers]. Anasthesiol Intensivmed Notfallmed Schmerzther. 1996 May;31(4):200-4. Review. German. Erratum in: Anasthesiol Intensivmed Notfallmed Schmerzther 1996 Nov;31(9):587. PubMed PMID: 8704077.
19: Shields JA. Heart block and prolonged Q-Tc interval following muscle relaxant reversal: a case report. AANA J. 2008 Feb;76(1):41-5. Review. PubMed PMID: 18323319.
20: Trepanier L. Acute vomiting in cats: rational treatment selection. J Feline Med Surg. 2010 Mar;12(3):225-30. doi: 10.1016/j.jfms.2010.01.005. Review. PubMed PMID: 20193913.
