Dolasetron

Dolasetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 20 nM). It is selective for 5-HT3 receptors over 5-HT1A, 5-HT1B, 5-HT2, dopamine D2, alpha1-, alpha2-, beta-adrenergic, M1-5 muscarinic acetylcholine, and neurokinin-1 (NK1) receptors (IC50s = >10 µM for all). Dolasetron inhibits 5-HT-induced membrane currents in NG 108-15 cells (IC50 = 3.8 nM). It increases the latency to emesis and reduces the number of vomiting and retching episodes induced by cisplatin (Cay-13119) in ferrets when administered at doses of 0.5 or 2 mg/kg. Formulations containing dolasetron have been used in the prevention of postoperative or chemotherapy-induced nausea.Formal Name: 1H-indole-3-carboxylic acid, octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester, stereoisomer. CAS Number: 115956-12-2. Synonyms: MDL 73147. Molecular Formula: C19H20N2O3. Formula Weight: 324.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 16 mg/ml. lambdamax: 213, 282 nm. SMILES: O=C1C2C[C@@](C[C@H](OC(C3=CNC4=C3C=CC=C4)=O)C[C@]5([H])C2)([H])[N@]5C1. InChi Code: InChI=1S/C19H20N2O3/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17/h1-4,9,11-14,20H,5-8,10H2/t11?,12-,13+,14+. InChi Key: UKTAZPQNNNJVKR-MMUVGSQPSA-N.