Dolasetron - CAS 115956-12-2
Catalog number:
115956-12-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H20N2O3
Molecular Weight:
324.37
COA:
Inquire
Targets:
5-HT Receptor
Description:
Dolasetron, a pseudopelletierine derivative, is a 5-HT3 receptor antagonist that could be used to relieve the nausea and vomiting caused by chemotherapy.
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Purity:
95%
Appearance:
White powder
Synonyms:
Dolasetron; UNII-82WI2L7Q6E; 82WI2L7Q6E; HSDB 7565; CHEMBL1237118
Solubility:
10 mM in DMSO
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
Dolasetron is a 5-HT3 receptor antagonist that could be used to relieve the nausea and vomiting caused by chemotherapy.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Boiling Point:
535.1ºC at 760 mmHg
Melting Point:
278ºC
Density:
1.37 g/cm3
InChIKey:
UKTAZPQNNNJVKR-UDXKHGJESA-N
InChI:
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?/m0/s1
Canonical SMILES:
C1C2CC3CC(CC1N3CC2=O)OC(=O)C4=CNC5=CC=CC=C54
1.Safety of an Oral Fixed Combination of Netupitant and Palonosetron (NEPA): Pooled Data From the Phase II/III Clinical Program.
Aapro M1, Hesketh PJ2, Jordan K3, Gralla RJ4, Rossi G5, Rizzi G5, Palmas M5. Oncologist. 2016 Apr;21(4):494-502. doi: 10.1634/theoncologist.2015-0301. Epub 2016 Mar 21.
BACKGROUND: Standard prophylaxis for chemotherapy-induced nausea and vomiting (CINV) with highly emetogenic and anthracycline-cyclophosphamide-based chemotherapy includes a 5-hydroxytryptamine-3 receptor antagonist, a neurokinin-1 receptor antagonist (NK1RA), and corticosteroid therapy. NEPA is a fixed combination of netupitant and palonosetron. The primary objective of this analysis was to document the safety profile, including cardiac safety, of NEPA + dexamethasone in comparison with current therapies across all phase II/III trials.
2.The modulation of carbonyl reductase 1 by polyphenols.
Boušová I1, Skálová L1, Souček P2, Matoušková P1. Drug Metab Rev. 2015;47(4):520-33. doi: 10.3109/03602532.2015.1089885. Epub 2015 Sep 29.
Carbonyl reductase 1 (CBR1), an enzyme belonging to the short-chain dehydrogenases/reductases family, has been detected in all human tissues. CBR1 catalyzes the reduction of many xenobiotics, including important drugs (e.g. anthracyclines, nabumetone, bupropion, dolasetron) and harmful carbonyls and quinones. Moreover, it participates in the metabolism of a number of endogenous compounds and it may play a role in certain pathologies. Plant polyphenols are not only present in many human food sources, but are also a component of many popular dietary supplements and herbal medicines. Many studies reviewed herein have demonstrated the potency of certain flavonoids, stilbenes and curcuminoids in the inhibition of the activity of CBR1. Interactions of these polyphenols with transcriptional factors, which regulate CBR1 expression, have also been reported in several studies. As CBR1 plays an important role in drug metabolism as well as in the protection of the organism against potentially harmful carbonyls, the modulation of its expression/activity may have significant pharmacological and/or toxicological consequences.
3.Implications of the IQ-CSRC Prospective Study: Time to Revise ICH E14.
Darpo B1, Garnett C, Keirns J, Stockbridge N. Drug Saf. 2015 Sep;38(9):773-80. doi: 10.1007/s40264-015-0325-5.
Exposure-response (ER) analysis has evolved as an important tool to evaluate the effect of a drug on cardiac repolarization, as reflected in the QTc interval. It has been suggested that careful electrocardiogram (ECG) evaluation in 'first-in-human' studies using ER analysis could replace or serve as an alternative to the E14 'thorough QT' study. This commentary shares and discusses the results of a recently conducted study with the objective to evaluate this approach. Six drugs with a well-characterized QT effect, five of which are known QT prolongers, were evaluated in a study design similar to a conventional single-ascending-dose study. Each drug was given to nine healthy subjects (six for placebo) in two dose levels, which for the positive drugs (ondansetron, quinine, dolasetron, moxifloxacin, and dofetilide) were chosen with the intent to cause 10-12 ms and 15-20 ms QTc prolongation. Replicate 12-lead ECGs were extracted from continuous recordings pre-dose and serially after dosing and paired with drug concentration determinations.
4.Comparative safety of serotonin (5-HT3) receptor antagonists in patients undergoing surgery: a systematic review and network meta-analysis.
Tricco AC1,2, Soobiah C3,4, Blondal E5, Veroniki AA6, Khan PA7, Vafaei A8, Ivory J9, Strifler L10, Ashoor H11, MacDonald H12, Reynen E13, Robson R14, Ho J15, Ng C16, Antony J17, Mrklas K18,19, Hutton B20, Hemmelgarn BR21, Moher D22, Straus SE23,24. BMC Med. 2015 Jun 18;13:142. doi: 10.1186/s12916-015-0379-3.
BACKGROUND: Serotonin (5-HT3) receptor antagonists are commonly used to decrease nausea and vomiting for surgery patients, but these agents may be harmful. We conducted a systematic review on the comparative safety of 5-HT3 receptor antagonists.
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Chemical Structure

CAS 115956-12-2 Dolasetron

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