Identification | Back Directory | [Name]
2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride | [CAS]
199864-86-3 | [Synonyms]
MT 500 Hydrochloride RS 127445 hydrochloride NEW 4-(4-Fluoro-1-naphthyl)-6-isopropylpyriMidin-2-aMine 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine hydrochloride 2-AMino-4-(4-fluoronaphth-1-yl)-6-isopropylpyriMidine Monohydrochloride 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine monohydrochloride 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride | [Molecular Formula]
C17H17ClFN3 | [MDL Number]
MFCD11112196 | [MOL File]
199864-86-3.mol | [Molecular Weight]
317.788 |
Hazard Information | Back Directory | [Uses]
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selec
tivity for this receptor as compared to numerous other receptor and ion channel binding sites. | [Biological Activity]
RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. | [in vivo]
In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration. RS-127445 is cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable[1]. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound[2]. | [IC 50]
sPLA2: 5.5 (pKi); 5-HT3 Receptor: <6 (pKi); 5-HT5 Receptor: <6 (pKi); 5-HT6 Receptor: <6 (pKi); 5-HT2A Receptor: 6.3 (pKi); 5-HT2C Receptor: 6.4 (pKi); 5-HT2B Receptor: 9.5 (pKi) | [storage]
Desiccate at +4°C |
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