Fesoterodine L-mandelate

Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK i 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) In Vitro Fesoterodine L-mandelate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Bladders from female Sprague-Dawley rats (225-275 g)Dosage: 0.01, 0.1 and 1 mg/kg Administration: IV Result: Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg. Form:Solid IC50& Target:pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)

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