rac Fesoterodine-d14 fumarate(Synonyms: 弗斯特罗定 d14 (富马酸盐))

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rac Fesoterodine-d14 fumarate (Synonyms: 弗斯特罗定 d14 (富马酸盐))

(Rac)-Fesoterodine-d14 fumarate 是 Fesoterodine 氘代消旋体。Fesoterodine 是一种口服有效，非亚型选择性的，竞争性毒蕈碱受体 (mAChR) 拮抗剂，对 M1，M2，M3，M4，M5 受体的 pKi 值分别为 8.0，7.7，7.4，7.3，7.5。Fesoterodine 用于膀胱过度活动症 (OAB)。

rac Fesoterodine-d14 fumarate(Synonyms: 弗斯特罗定 d14 (富马酸盐))

rac Fesoterodine-d14 fumarate Chemical Structure

CAS No. : 1185237-08-4

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生物活性

(Rac)-Fesoterodine-d14 fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB)[1][2].

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[1].

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

541.74

Formula

C30H27D14NO7
CAS 号

1185237-08-4
中文名称

弗斯特罗定 d14 (富马酸盐)
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):211-216.

    [2]. Ellsworth P, et al. Fesoterodine for the treatment of urinary incontinence and overactive bladder. Ther Clin Risk Manag. 2009;5:869-76. Epub 2009 Nov 18.

    [3]. Didem Yilmaz-Oral, et al. The Beneficial Effect of Fesoterodine, a Competitive Muscarinic Receptor Antagonist on Erectile Dysfunction in Streptozotocin-induced Diabetic Rats

    [4]. Peter Ney, et al. Pharmacological Characterization of a Novel Investigational Antimuscarinic Drug, Fesoterodine, in Vitro and in Vivo. BJU Int. 2008 Apr;101(8):1036-42.

    [5]. Martin C Michel, et al. Fesoterodine: A Novel Muscarinic Receptor Antagonist for the Treatment of Overactive Bladder Syndrome. Expert Opin Pharmacother. 2008 Jul;9(10):1787-96.

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