Fesoterodine L-mandelateFesoterodine L-mandelate
MedChemExpress (MCE)
HY-70053A
1206695-46-6
99.00%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
Fesoterodine L-mandelate 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 L-mandelate is used for the overactive bladder (OAB).
Fesoterodine L-mandelate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition[1]. After oral administration, Fesoterodine L-mandelate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine
SPM 7605
HY-76569
an active metabolite of Fesoterodine)[3][4].
Fesoterodine L-mandelate (0.01-1 mg/kg
IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg[3].
mAChR1 mAChR3 mAChR4 mAChR5
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[1]. 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. [Content Brief]
[2]. Didem Yilmaz-Oral, et al. The Beneficial Effect of Fesoterodine, a Competitive Muscarinic Receptor Antagonist on Erectile Dysfunction in Streptozotocin-induced Diabetic Rats [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]