Tegaserod-13C,d3 maleate(Synonyms: SDZ-HTF-919-13C,d3; HTF-919-13C,d3)

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Tegaserod-13C,d3 maleate (Synonyms: SDZ-HTF-919-13C,d3; HTF-919-13C,d3)

Tegaserod-13C,d3 (maleate) 是一种 13C- 和氘代标记的 Tegaserod (maleate)。Tegaserod maleate 是选择性的、5-HT4 受体的部分激动剂和 5-HT2B 受体的拮抗剂。Tegaserod maleate 在胃肠道中表现出促进的作用。

Tegaserod-13C,d3 maleate(Synonyms: SDZ-HTF-919-13C,d3; HTF-919-13C,d3)

Tegaserod-13C,d3 maleate Chemical Structure

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生物活性

Tegaserod-13C,d3 (maleate) is the 13C- and deuterium labeled. Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[50].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

421.47

Formula

C1913CH24D3N5O5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

    [2]. A E Vickers, et al. In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Drug Metab Dispos. 2001 Oct;29(10):1269-76.

    [3]. T C Seerden, et al. Experimental pancreatitis disturbs gastrointestinal and colonic motility in mice: effect of the prokinetic agent tegaserod. Neurogastroenterol Motil. 2007 Oct;19(10):856-64.

    [4]. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43.

    [5]. H-C Pan, et al. Tegaserod, a small compound mimetic of polysialic acid, promotes functional recovery after spinal cord injury in mice. Neuroscience. 2014 Sep 26;277:356-66.

    [6]. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60.

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