CAS 286930-02-7|Fesoterodine

Introduction:Basic information about CAS 286930-02-7|Fesoterodine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameFesoterodine
CAS Number286930-02-7Molecular Weight412.58500
Density1.043Boiling Point518.9ºC at 760 mmHg
Molecular FormulaC26H37NO3Melting Point/
MSDS/Flash Point267.6ºC

Names

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

Fesoterodine BiologicalActivity

DescriptionFesoterodine 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 CatalogSignaling Pathways >>Neuronal Signaling >>mAChRSignaling Pathways >>GPCR/G Protein >>mAChRResearch Areas >>Metabolic DiseaseResearch Areas >>Neurological Disease
Target

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

In VitroFesoterodine 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 VivoFesoterodine (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

Density1.043
Boiling Point518.9ºC at 760 mmHg
Molecular FormulaC26H37NO3
Molecular Weight412.58500
Flash Point267.6ºC
Exact Mass412.28500
PSA49.77000
LogP5.48800
InChIKeyDCCSDBARQIPTGU-HSZRJFAPSA-N
SMILESCC(C)C(=O)Oc1ccc(CO)cc1C(CCN(C(C)C)C(C)C)c1ccccc1

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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