Palonosetron (hydrochloride)

Palonosetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.04 nM). 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 (Cay-13119), dacarbazine (Cay-21877), actinomycin D (Cay-11421), and mechlorethamine in dogs (ID50s = 1.9, 4.1, 4.9, and 4.4 µg/kg, respectively). Formulations containing palonosetron have been used in the treatment of postoperative or chemotherapy-induced nausea and vomiting.Formal Name: 2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3aS,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one, monohydrochloride. CAS Number: 135729-62-3. Synonyms: RS 25259-197. Molecular Formula: C19H24N2O . HCl. Formula Weight: 332.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 210, 239 nm. SMILES: O=C(N([C@H]1C(CC2)CCN2C1)C3)C4=CC=CC5=C4[C@]3([H])CCC5.Cl. InChi Code: InChI=1S/C19H24N2O.ClH/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20,/h2,4,6,13,15,17H,1,3,5,7-12H2,1H/t15-,17-,/m1./s1. InChi Key: OLDRWYVIKMSFFB-SSPJITILSA-N.