| Name | Fesoterodine fumarate |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.25 mM), Sonication is recommended.
DMSO : 93 mg/mL (176.25 mM), Sonication is recommended.
H2O : 92 mg/mL (174.36 mM), Sonication is recommended.
Ethanol : 93 mg/mL (176.25 mM), Sonication is recommended.
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| Keywords | SPM-907 | SPM907 | SPM7605 | receptor | overactive | orally | OAB | Muscarinic acetylcholine receptor | muscarinic | mAChR | Inhibitor | inhibit | Fesoterodine Fumarate | Fesoterodine | Desfesoterodine | bladder | antimuscarinic | 5-HMT |
| Inhibitors Related | Adiphenine hydrochloride | Levamisole hydrochloride | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Hexamethonium Bromide | Ribavirin | Adenine | Mitotane | Choline chloride | Propoxur | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Approved Drug Library | Membrane Protein-targeted Compound Library | Drug-induced Liver Injury (DILI) Compound Library | EMA Approved Drug Library | Anti-Parkinson's Disease Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
