Fesoterodine Fumarate 是可口服的，非亚型选择性的竞争性毒蕈碱受体拮抗剂，用于膀胱过度活动症，对 M1、M2、M3、M4 和 M5 受体的pKi值分别为 8.0、7.7、7.4、7.3 和 7.5。

Fesoterodine Fumarate 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.

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]

286930-03-8

C26H37NO3·C4H4O4

527.65

SPM 907;富马酸非索罗定;Toviaz;Fesoterodine fumarate

DMSO:93 mg/mL (176.3 mM)
Ethanol:93 mg/mL (176.3 mM)
H2O:92 mg/mL (174.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years