Fesoterodine

Modify Date: 2024-01-11 12:30:12

Fesoterodine Structure
Fesoterodine structure
Common Name Fesoterodine
CAS Number 286930-02-7 Molecular Weight 412.58500
Density 1.043 Boiling Point 518.9ºC at 760 mmHg
Molecular Formula C26H37NO3 Melting Point N/A
MSDS N/A Flash Point 267.6ºC

 Use of 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].

 Names

Name [2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate
Synonym More Synonyms

 Fesoterodine Biological Activity

Description 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
Target

pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)[3]

In Vitro Fesoterodine decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition[1]. After oral administration, Fesoterodine 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].
In Vivo Fesoterodine (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]. Animal Model: Bladders from female Sprague-Dawley rats (225-275 g)[3] 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.
References

[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.

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

[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.

[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.

 Chemical & Physical Properties

Density 1.043
Boiling Point 518.9ºC at 760 mmHg
Molecular Formula C26H37NO3
Molecular Weight 412.58500
Flash Point 267.6ºC
Exact Mass 412.28500
PSA 49.77000
LogP 5.48800

 Synthetic Route

 Synonyms

(R)-2-(3-N,N-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenoxyisobutyrate
(R)-(+)-isobutyric acid 2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl ester
2-methyl propanoic acid 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-(hydroxymethyl) phenyl ester
isobutyric acid 2-((R)-3-diisopropylanimonium-1-phenylpropyl)-4-(hydroxymethyl)phenyl ester
(R)-Fesoterodine fumarate
Fesoterodine (INN)
FESO
2-[(1R)-3-(dipropan-2-ylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate
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