Palonosetron-d3 is intended for use as an internal standard for the quantification of palonosetron by GC- or LC-MS. Palonosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.04 nM).1 It is selective for 5-HT3 over 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kis = ≥15.85 μM for all), as well as a panel of additional neurotransmitter receptors. Palonosetron inhibits 5-HT-induced contraction in isolated guinea pig ileum. It inhibits cisplatin-induced emesis in ferrets (ID50 = 1.1 μg/kg, i.v.) as well as emesis induced by cisplatin , dacarbazine , actinomycin D , and mechlorethamine in dogs (ID50s = 1.9, 4.1, 4.9, and 4.4 μg/kg, respectively).2 Formulations containing palonosetron have been used in the treatment of postoperative or chemotherapy-induced nausea and vomiting.
|1. Wong, E.H., Clark, R., Leung, E., et al. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br. J. Pharmacol. 114(4), 851-859 (1995).|2. Eglen, R.M., Lee, C.H., Smith, W.L., et al. Pharmacological characterization of RS 25259-197, a novel and selective 5-HT3 receptor antagonist, in vivo. Br. J. Pharmacol. 114(4), 860-866 (1995).