الصفحة الرئيسية>>Signaling Pathways>> Neuroscience>> mAChR>>(R)-(+)-Tolterodine

(R)-(+)-Tolterodine

رقم الكتالوجGC11219

(R) - (+) -Tolterodine (PNU-200583) هو أحد مضادات مستقبلات المسكارينية القوية التي تظهر انتقائية للمثانة البولية على الغدد اللعابية في الجسم الحي.

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(R)-(+)-Tolterodine التركيب الكيميائي

Cas No.: 124937-51-5

الحجم السعر المخزون الكميّة
1g
341٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (R)-(+)-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: mAChRin 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].

References:
[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.

Chemical Properties of (R)-(+)-Tolterodine

Cas No. 124937-51-5 SDF
Chemical Name 2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol
Canonical SMILES CC1=CC(=C(C=C1)O)C(CCN(C(C)C)C(C)C)C2=CC=CC=C2
Formula C22H31NO M.Wt 325.49
الذوبان Ethanol : 120 mg/mL (368.67 mM; Need ultrasonic); DMSO : 100 mg/mL (307.23 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (R)-(+)-Tolterodine

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1 mg 5 mg 10 mg
1 mM 3.0723 mL 15.3615 mL 30.7229 mL
5 mM 0.6145 mL 3.0723 mL 6.1446 mL
10 mM 0.3072 mL 1.5361 mL 3.0723 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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