Tolterodine

Research use only, not for human use.

Tolterodine ((R)-(+)-Tolterodine) is a novel and selective muscarinic-type receptor (mAChR) antagonist used in the treatment of detrusor instability and overactive bladder syndrome.

Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. IC50 Value:Target: mAChR in vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM).The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors .in vivo: Tolterodine was extensively metabolized in vivo .In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased .

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Cell Cycle/DNA Damage

AChR

AChR

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124937-51-5

325.49

C22H31NO

>98% (HPLC)

In Vitro:?Ethanol : 120 mg/mL (368.67 mM; Ultrasonic)DMSO : 100 mg/mL (307.23 mM; Ultrasonic )

[C@H](CCN(C(C)C)C(C)C)(C1=C(O)C=CC(C)=C1)C2=CC=CC=C2

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(-20℃)

With Ice Pack

≥ 2 years