Tolterodine

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].

124937-51-5

(R) - (+) -Tolterodine; (+) -Tolterodine; (R) -Tolterodine; PNU-200583

12352005

H302, H312, H332

MAChR

Reference compound

GPCR/G Protein; Neuronal Signaling

Neuroscience-Neuromodulation

Neurological Disease; Cancer

https://www.medchemexpress.com/Tolterodine.html

98.63

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 120 mg/mL (ultrasonic)

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

C22H31NO

325.49

H302, H312, H332

[1]Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90 (5) :260-7.|[2]Andersson SH, et al. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26 (6) :528-35.|[3]Cappon GD, et al. Tolterodine does not affect memory assessed by passive-avoidance response test in mice. Eur J Pharmacol. 2008 Jan 28;579 (1-3) :225-8.

Blue Ice

-20°C, 3 years (Powder)

Reference compound1