2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶

发布者：信康浏览次数：

产品名称:2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶

CAS:199864-87-4

别名：2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶;2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶盐酸盐;RS-127445盐酸盐;4-(4-氟-1-萘)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐;游离的CAS号87-4

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

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生物活性RS-127445是一种选择性5-HT2B受体拮抗剂，pK_i为9.5，pIC50为10.4，比作用于其他5-HT受体选择性高1000倍以上。
体外研究RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine.
体内研究RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are achieved are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. . RS-127445 inhibits colonic motility and defecation.