Desfesoterodine 是选择性毒蕈碱受体拮抗剂，Kb和pA2分别为 0.84 nM 和 9.14。它可改善大鼠脑梗死诱导膀胱过度活动，是 Tolterodine 和 Fesoterodine 的主要药理活性代谢产物。

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. [1] 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3]

5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. [1]

207679-81-0

C22H31NO2

341.495

PNU-200577;(R)-5-Hydroxymethyl Tolterodine;5-hydroxymethyl Tolterodine;(R)-5-羟甲基托特罗定;5-HMT;5-HM;Desfesoterodine

Ethanol:63 mg/mL (184.5 mM)
DMSO:63 mg/mL (184.5 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years