Granisetron (hydrochloride)

Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT₃ (K_i = 3.9 nM) with antiemetic activity.^1,2 It is selective for 5-HT₃ over 5-HT₄ receptors (K_i = >1,000 nM).¹ Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).² It also increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) 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.

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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 receptors. J. 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 emesis. Jpn. J. Pharmacol. 63(3), 377-383 (1993).