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Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $77 | In Stock | |
25 mg | $113 | In Stock | |
50 mg | $155 | In Stock | |
100 mg | $239 | In Stock | |
500 mg | $463 | In Stock | |
1 mL x 10 mM (in DMSO) | $55 | In Stock |
Description | Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine. |
In vitro | Fesoterodine is rapidly and extensively converted to 5-HMT, such that the pharmacologic activity appears to be primarily attributable to 5-HMT. [1] Fesoterodine is a competitive antagonist of cholinergic agonist-stimulated responses in human M1-M5 cell lines and has a similar potency and selectivity profile to the radioligand-binding studies. Fesoterodine causes a rightward shift of the concentration-response curve for carbachol with no depression of the maximum in rat bladder strips, and concentration-dependently reduces contractions induced by electrical field stimulation (EFS). [2] Fesoterodine is hydrolyzed by nonspecific esterases to 5-hydroxmethyl tolterodine (5-HMT), which is the active metabolite and is responsible for all its antimuscarinic activity. [3] |
Alias | Toviaz, SPM 907 |
Molecular Weight | 527.65 |
Formula | C26H37NO3·C4H4O4 |
Cas No. | 286930-03-8 |
Smiles | OC(=O)C=CC(O)=O.CC(C)N(CCC(C1=CC=CC=C1)C1=C(OC(=O)C(C)C)C=CC(CO)=C1)C(C)C |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (176.3 mM) H2O: 92 mg/mL (174.4 mM) Ethanol: 93 mg/mL (176.3 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO/Ethanol
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