A 5-HT3 receptor antagonist (Ki = 20 nM in a radioligand binding assay); reversibly suppresses 5-HT-induced membrane current in voltage-clamped NGI108-15 cells (IC50 = 3.8 nM); is a prodrug that is metabolized by carbonyl reductase to form reduced dolasetron

Dolasetron – 50 mg

Brand:
Cayman
CAS:
115956-12-2
Storage:
-20
UN-No:
Non-Hazardous - /

Dolasetron is a potent antagonist of the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 20 nM in a radioligand binding assay.{40077} It reversibly suppresses 5-HT-induced membrane current in voltage-clamped NGI108-15 cells (IC50 = 3.8 nM). Dolasetron is a prodrug that is metabolized by carbonyl reductase to form reduced dolasetron, the major pharmacologically active metabolite in humans.{40078} Formulations containing dolasetron are under investigation for utility in treating chemotherapy-induced nausea and vomiting.{40079}  

 

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Description

A 5-HT3 receptor antagonist (Ki = 20 nM in a radioligand binding assay); reversibly suppresses 5-HT-induced membrane current in voltage-clamped NGI108-15 cells (IC50 = 3.8 nM); is a prodrug that is metabolized by carbonyl reductase to form reduced dolasetron, the major pharmacologically active metabolite in humans

Formal name: 1H-indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, stereoisomer

Synonyms:  MDL 73147

Molecular weight: 324.4

CAS: 115956-12-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience

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