Rac-Fesoterodine-d14 (fumaraat)

(Rac) -Fesoterodine-d14 fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKivalues 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].

1185237-08-4

12352005

Isotope-Labeled Compounds; mAChR

GPCR/G Protein; Neuronal Signaling; Others

Metabolism-sugar/lipid metabolism

Metabolic Disease; Neurological Disease

10 mM in DMSO

C(=CC(O)=O)C(O)=O.C(CCN(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])[2H])C(C([2H])([2H])[2H])(C([2H])([2H])[2H])[2H])(C1=C(OC(C(C)C)=O)C=CC(CO)=C1)C2=CC=CC=C2

C30H27D14NO7

541.74

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-70053S/

Isotope-Labeled Compounds

No Development Reported

MAChR1; mAChR3; mAChR4; mAChR5