(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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 124937-51-5
Sample solution is provided at 25 µL, 10mM.
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
(Based on Reviews and 11 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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