Dolasetron-d4 (Synonyms: MDL-73147-d4)

Dolasetron-d₄ is intended for use as an internal standard for the quantification of dolasetron by GC- or LC-MS. Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT₃ (K_i = 20 nM).¹ It is selective for 5-HT₃ receptors over 5-HT_1A, 5-HT_1B, 5-HT₂, dopamine D₂, α₁-, α₂-, and β-adrenergic, M_1-5 muscarinic acetylcholine, and neurokinin-1 (NK₁) receptors (IC₅₀s = >10 µM for all).² Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC₅₀ = 3.8 nM).¹ It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin in ferrets when administered at doses of 0.5 or 2 mg/kg.² Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.

1.Beoijinga, P.H., Galvan, M., Baron, B.M., et al.Characterization of the novel 5-HT3 antagonists MDL 73147EF (dolasetron mesilate) and MDL 74156 in NG108-15 neuroblastoma x glioma cellsEur. J. Pharmacol.219(1)9-13(1992) 2.Miller, R.C., Galvan, M., Gittos, M.W., et al.Pharmacological properties of dolasetron, a potent and selective antagonist at 5-HT3 receptorsDrug Develop. Res.28(1)87-93(1993)