Description
Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT
3 (K
i = 20 nM). It is selective for 5-HT
3 receptors over 5-HT
1A, 5-HT
1B, 5-HT
2, dopamine D
2, α
1-, α
2-, β-adrenergic, M
1-5 muscarinic acetylcholine, and neurokinin-1 (NK
1) receptors (IC
50s = >10 μM for all). Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC
50 = 3.8 nM). 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. Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.
