4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
RS-127445
CAS: 199864-87-4
Molecular Formula: C17H16FN3
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE - Names and Identifiers
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C17H16FN3 |
| Molar Mass | 281.33 |
| Density | 1.213 |
| Boling Point | 472.8℃ at 760 mmHg |
| Storage Condition | Inert atmosphere,2-8°C |
| In vitro study | RS-127445 is a novel high-affinity, selective 5-HT2B receptor antagonist that lacks detectable intrinsic activity. RS-127445 has nanomolar affinity and 1000-fold selectivity for the 5-HT2B receptor. Thus RS-127445 has the highest affinity and selectivity for the 5-HT2B receptor ligand. RS-127445 effectively blocked the 5-ht-induced increase in inositol phosphate formation and the 5-ht-induced increase in intracellular calcium concentration with a 1000-fold greater potency than yohimbine. |
| In vivo study | RS-127445 is readily absorbed, has no apparent dose or route-dependent limits, is rapidly absorbed after oral and intraperitoneal administration, and maximum plasma concentrations are achieved within 15 minutes of administration. The concentration of RS-127445 in the plasma is directly proportional to the administered dose. RS-127445 administered at a dose of 5 mg/kg, approximately 60% of the intraperitoneal dose and 14% of the oral dose are bioavailable. The concentration of RS-127445 in plasma is expected to fully saturate the accessible 5-HT2B receptor, which can be readily achieved and maintained in rats. Oral administration of RS-127445 at 1 to 10 mg/kg significantly inhibited restraint stress-induced visceral hypersensitivity by up to 35 to 74%. Oral administration of RS-127445 significantly inhibited TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/kg), although RS-127445 had no significant effect on the nociceptive threshold of native rat viscera. RS-127445 administered orally at 1 to 30 mg/kg dose-dependently reduced restraint stress-induced defecation in naïtive and TNBS-treated rats. RS-127445 inhibits colon motility and defecation. |
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View History
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
2-TERT-BUTYL-7-METHYL-1H-INDOLE
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2-(4-甲基-1H-咪唑-5-基)乙烷-1-胺
BENZYLOXYCARBONYL-D-ASPARTIC ACID
FMOC-L-GLUTAMIC ACID-GAMMA-METHYL ESTER
1H-Pyrazol-4-ol, 1-methyl-3,5-bis(3-methylphenyl)-
2,2-二氟-2-[2-(丙烷-2-氧基)苯基]乙酸
2-TERT-BUTYL-7-METHYL-1H-INDOLE
Pyrido[2,3-b]pyrazine, 7-chloro-
2-(2-氯噻唑-5-基)乙酸乙酯
乙酰苯那嗪-D4二马来酸酯
2-(4-甲基-1H-咪唑-5-基)乙烷-1-胺
BENZYLOXYCARBONYL-D-ASPARTIC ACID
FMOC-L-GLUTAMIC ACID-GAMMA-METHYL ESTER
1H-Pyrazol-4-ol, 1-methyl-3,5-bis(3-methylphenyl)-
2,2-二氟-2-[2-(丙烷-2-氧基)苯基]乙酸