rac Fesoterodine-d14 Fumarate

Names

[ CAS No. ]:
1185237-08-4

[ Name ]:
rac Fesoterodine-d14 Fumarate

[Synonym ]:
[2-[3-[bis(1,1,1,2,3,3,3-heptadeuteriopropan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate,(E)-but-2-enedioic acid

Biological Activity

[Description]:

(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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease

[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H27D14NO7

[ Molecular Weight ]:
541.73500

[ Exact Mass ]:
541.37600

[ PSA ]:
124.37000

[ LogP ]:
5.09290

Related Compounds