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 [1]. in vivo: Tolterodine was extensively metabolized in vivo [2]. 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 [3].
Molekulargewicht:
325.49
Reinheit:
98.63
CAS Nummer:
[124937-51-5]
Formel:
C22H31NO
Target-Kategorie:
mAChR
Anwendungsbeschreibung:
MCE Product type: Reference compound
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