Granisetron (hydrochloride)

Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity. It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM). 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 (Cay-13119). 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 (Cay-15007) and cyclophosphamide (Cay-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.Formal Name: 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide, monohydrochloride. CAS Number: 107007-99-8. Synonyms: BRL 43694. Molecular Formula: C18H24N4O . HCl. Formula Weight: 348.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Ethanol: slightly, PBS (pH 7.2): 10 mg/ml, Water: miscible. lambdamax: 208, 301 nm. SMILES: CN1[C@H]2C[C@H](NC(C3=NN(C)C4=C3C=CC=C4)=O)C[C@@H]1CCC2.Cl. InChi Code: InChI=1S/C18H24N4O.ClH/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17,/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23),1H/t12-,13+,14-,. InChi Key: QYZRTBKYBJRGJB-WQTKJZBYSA-N.