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Dolasetron

Cat. No. M20473
Dolasetron Structure
Synonym:

MDL-73147

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Biological Activity

Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.

Chemical Information
Molecular Weight 324.37
Formula C19H20N2O3
CAS Number 115956-12-2
Solubility (25°C) DMSO 64 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Dolasetron

[2] Stephanie Weibel, et al. Cochrane Database Syst Rev. Drugs for preventing postoperative nausea and vomiting in adults after general anaesthesia: a network meta-analysis

[3] No authors listed. Anesth Analg. Dolasetron for preventing postanesthetic shivering: Retraction

[4] Martin Rochford, et al. Emerg Med J. Dolasetron overdose resulting in prolonged QTc interval and severe hypotension: a case report and literature review

[5] J A Balfour, et al. Drugs. Dolasetron. A review of its pharmacology and therapeutic potential in the management of nausea and vomiting induced by chemotherapy, radiotherapy or surgery

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