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

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Struktur
199864-87-4
CAS-Nr.
199864-87-4
Englisch Name:
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
Synonyma:
445;MT500;RS127;RS 127;RS-127;RS127445;RS-127445HCl;RS 127445 hydrochlor;RS 127445 HYDROCHLORIDE;2,7-Naphthyridin-1(8H)-one
CBNumber:
CB92456354
Summenformel:
C17H16FN3
Molgewicht:
281.33
MOL-Datei:
199864-87-4.mol

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

Dichte
1.213
storage temp. 
Inert atmosphere,2-8°C
Löslichkeit
≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
Aggregatzustand
solid

Sicherheit

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

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

Biologische Aktivität

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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199864-87-4()Verwandte Suche:


  • 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
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