Granisetron-d3 is intended for use as an internal standard for the quantification of granisetron by GC- or LC-MS. Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.1,2 It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).1 Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to a first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin .2 It also increases the latency to a first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin and cyclophosphamide when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.
1.LÓpez-RodrÍguez, M.L., BenhamÚ, B., Morcillo, M.J., et al.Benzimidazole derivatives. 2. Synthesis and structure-activity relationships of new azabicyclic benzimidazole-4-carboxylic acid derivatives with affinity for serotoninergic 5-HT3 receptorsJ. Med. Chem.42(24)5020-5028(1999) 2.Haga, K., Inaba, K., Shoji, H., et al.The effects of orally administered Y-25130, a selective serotonin3-receptor antagonist, on chemotherapeutic agent-induced emesisJpn. J. Pharmacol.63(3)377-383(1993)