Tropisetron (hydrochloride)

Tropisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.8 nM for the mouse receptor). It is selective for 5-HT3 over the 5-HT4 receptor subtype (Ki = 156 nM for the porcine receptor). Tropisetron is also an antagonist of the alpha9 nicotinic acetylcholine receptor (nAChR, IC50 = 166 nM for the rat receptor) and a partial agonist of the alpha7 nAChR (Ki = 6.9 nM for the rat receptor). It enhances glycine-induced potentiation of homomeric alpha1 but not homomeric alpha2 glycine receptors when used at a concentration of 10 µM. Tropisetron (0.1 nM) blocks 5-HT-induced depolarizations in isolated rabbit nodose ganglia. It exhibits anti-emetic effects in a ferret model of emesis induced by cisplatin (Cay-13119) when administered at a dose of 1 mg/kg. Formulations containing tropisetron have been used in the treatment of nausea and vomiting associated with chemotherapy.Formal Name: 1H-indole-3-carboxylic acid (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester, monohydrochloride. CAS Number: 105826-92-4. Synonyms: ICS 205-930, SDZ-ICS 930. Molecular Formula: C17H20N2O2 . HCl. Formula Weight: 320.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Ethanol: slightly, PBS (pH 7.2): 10 mg/ml. lambdamax: 213, 228, 281 nm. SMILES: CN1[C@@H]2C[C@@H](OC(C3=CNC4=C3C=CC=C4)=O)C[C@H]1CC2.Cl. InChi Code: InChI=1S/C17H20N2O2.ClH/c1-19-11-6-7-12(19)9-13(8-11)21-17(20)15-10-18-16-5-3-2-4-14(15)16,/h2-5,10-13,18H,6-9H2,1H3,1H/t11-,12+,13+,. InChi Key: XIEGSJAEZIGKSA-LUNMCBQDSA-N.