RS-127445

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Chemical Structure| 199864-87-4 同义名 : MT500
CAS号 : 199864-87-4
货号 : A654799
分子式 : C17H16FN3
纯度 : 99%+
分子量 : 281.33
MDL号 : MFCD20270616
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
生物活性
靶点

  • 5-HT2

    5-HT2B, pIC50:10.4

    5-HT2B, pKi:9.5
描述 RS-127445, a selective, high anity, orally bioavailable 5-HT2B receptor antagonist. RS-127445 potently displaced [3H]-5-HT from human recombinant 5-HT2B receptor expressed in CHO-K1 cells. The anity (pKi value) of RS-127445 for the 5-HT2B receptor was 9.5+0.1. In vitro research suggests RS-127445 potently inhibited the 5-HT evoked increase in the formation of inositol phosphates in cells expressing 5-HT2B receptor. RS-127445 potently blocked the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK293 cells expressing the 5-HT2B receptor (pIC50 value of 10.4+0.1). RS-127445 potently blocked the 5-HT evoked contraction of the isolated fundus. Peak plasma concentrations were 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[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.55mL

7.11mL

3.55mL
参考文献

[1]Ohashi-Doi K, Himaki D, et al. A selective, high affinity 5-HT 2B receptor antagonist inhibits visceral hypersensitivity in rats. Neurogastroenterol Motil. 2010 Feb;22(2):e69-76.

[2]Bonhaus DW, Flippin LA, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82.

[3]Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82. doi: 10.1038/sj.bjp.0702632. PMID: 10455251; PMCID: PMC1566110.