RS-127445 , 98% , 199864-87-4

Synonym(s):
2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine hydrochloride

CAS NO.：199864-87-4

Empirical Formula: C17H16FN3

Molecular Weight: 281.33

MDL number: MFCD20270616

PRODUCT Properties

• Density: 1.213
• storage temp.: Inert atmosphere,2-8°C
• solubility: ≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
• form: solid
• color: White to off-white

Description and Uses

RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT_2B (K_i = 0.32 nM). It is selective for 5-HT_2B over other 5-HT receptor subtypes (K_i = >3 μM for 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C, 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 . It also blocks (±)-α-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 (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.

RS-127445 is a 5-HT2B receptor antagonist with modest activity against other 5-HT receptors. Selective 5-HT2B receptor antagonist

Safety

• Symbol(GHS): GHS06
• Signal word: Danger
• Hazard statements: H301-H315-H319-H335-H413
• Precautionary statements: P264-P270-P301+P310-P321-P330-P405-P501-P280-P302+P352-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P273