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RS 127445
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RS 127445图片
CAS NO:199864-87-4
规格:98%
分子量:281.33
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
5-HT2B receptor antagonist,high affinity
CAS:199864-87-4
分子式:C17H16FN3
分子量:281.33
纯度:98%
存储:Store at -20°C

Background:

RS-127445(MT 500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4 [1].


5-HT2B receptor belongs to the 5-HT2 receptor family which binds the neurotransmitter serotonin. It plays important role relevant to serotonin, including neuronal sensitization to tactile stimuli.


RS 127445 is a selective serotonin 5-HT2B receptor inhibitor. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor [2]. 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.


In rat model, oral administration of RS-127445 at 1 to 10 mg/kg resulted in significant inhibition of visceral hypersensitivity up to 35 to 74% triggered by restraint stress [3]. Moreover, 3 to 30 mg/ kg of RS-127445 resulted in a significant inhibition of TNBS-induced visceral hypersensitivity varied from 15 to 62% [3].


参考文献:
[1].  O'Mahony, S M et al. 5-HT2B receptors modulate visceral hypersensitivity in a stress-sensitive animal model of brain-gut axis dysfunction. Neurogastroenterology & Motility, 2012, 22(5): 573-578.
[2].  Ohashi-Doi K et al. A selective, high affinity 5-HT2B receptor antagonist inhibits visceral hypersensitivity in rats. Neurogastroenterology & Motility, 2010, 22(2): 69-76.
[3].  Bassil A K et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. British Journal of Pharmacology, 2009, 158(1): 252-258.