ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Neuronal Signaling >5-HT Receptor Antagonists >4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Structure
CAS No.
199864-87-4
Chemical Name:
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
Synonyms
445;MT500;RS127;RS 127;RS-127;RS127445;RS-127445HCl;RS 127445 hydrochlor;RS 127445 HYDROCHLORIDE;2,7-Naphthyridin-1(8H)-one
CBNumber:
CB92456354
Molecular Formula:
C17H16FN3
Molecular Weight:
281.33
MOL File:
199864-87-4.mol
Modify Date:
2024/7/2 8:55:41

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE 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

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Chemical Properties,Uses,Production

Description

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 . 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.

Uses

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

Biological Activity

High affinity 5-HT 2B receptor antagonist (pK i = 9.5). Displays 1000-fold selectivity for 5-HT 2B with good bioavailability.

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Spectrum

199864-87-4(4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE)Related Search:

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE RS 127445 HYDROCHLORIDE 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine MT500 RS127445 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)- 4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyriMidin-2-aMine hydrochloride RS-127445HCl 4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine RS 127445 hydrochloride,4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinaminehydrochloride RS 127 RS127 RS-127 RS-127445;RS 127445;RS127445;RS127;445;RS 127;445;RS-127;445 Ziprasidone4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE MT500;MT 500;RS 127445;RS127445;RS127;445;RS 127;445;RS-127;445 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE USP/EP/BP 445 4-(4-fluoronaphthalen-1-yl)-6-propan-2-ylpyrimidin-2-amine RS 127445 hydrochlor 2,7-Naphthyridin-1(8H)-one 199864-87-4 199864-87-3 C17H17ClFN3 C17H16FN3HCl Inhibitors