Dolasetronmesylate , 10mMinDMSO , 115956-13-3

Synonym(s):
Anzemet hydrate;Dolasetron mesylate monohydrate;Dolasetron methanesulfonate;Dolasetron methanesulfonate hydrate

CAS NO.：115956-13-3

Empirical Formula: C20H26N2O7S

Molecular Weight: 438.49

MDL number: MFCD01718979

EINECS: 601-404-5

PRODUCT Properties

• Melting point: 278°
• storage temp.: Sealed in dry,2-8°C
• solubility: H2O: >30mg/mL
• form: powder
• color: white to off-white
• CAS DataBase Reference: 115956-13-3(CAS DataBase Reference)

Description and Uses

Dolasetron was launched as Anzemet in Australia and the US for the prevention of nausea and vomiting in chemotherapy patients. It is a highly potent and very selective antagonist of 5-HT3 receptors ; it is the sixth in this class of compounds to be marketed for the treatment of chemotherapy-induced emesis. The last two approved in this class were Nazasetron (1994) and Ramosetron (1996). Anzemet was prepared by a seven step sequence from a cyclopentenecarboxylic ester via a Robinson-Schopf cyclisation of a dialdehyde into a key 9-azabicyclo[3.3.l]nonan-3-one. In a clinical study with 164 cancer patients treated with Dolasetron mesylate prior to Cisplatin, single doses of 10- 50 mg achieved major control of nausea and emesis in 73% of subjects and were well tolerated. Results from pharmacokinetic studies in humans showed that the clinical effects and duration of action seem to be due mainly to a major plasma metabolite rapidly formed and very potent itself, the (+) enantiomeric alcohol obtained by enzymatic reduction of the cyclic ketone.

Dolasetron Mesylate acts as a bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Antiemetic.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338
• WGK Germany: 3