RS 127445 (hydrochloride)

RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM). It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 µM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT (Cay-14332). It also blocks (±)-alpha-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner. Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Cay-ISO60176, Cay-16186, Cay-22165) or quinpirole.Formal Name: 4-(4-fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine, monohydrochloride. CAS Number: 199864-86-3. Molecular Formula: C17H16FN3 . HCl. Formula Weight: 317.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 223, 309 nm. SMILES: FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=C1C=CC=C3.Cl. InChi Code: InChI=1S/C17H16FN3.ClH/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13,/h3-10H,1-2H3,(H2,19,20,21),1H. InChi Key: MKJPYBJBPRFMHL-UHFFFAOYSA-N.