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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Tolterodine tartrate (PNU-200583E; PNU200583E; Detrol LA; Detrusitol) is a tartrate salt of tolterodine that is a potent and competitive muscarinic receptor antagonist. Tolterodines is an antimuscarinic drug that has been used for symptomatic treatment of urinary incontinence. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors. Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M3 and M1 selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body.
ln Vitro |
Both tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM) were found to be effective in inhibiting the contractions of the isolated guinea pig bladder caused by carbachol. The antimuscarinic potency of tolterodine was 27, 200, and 370–485, times higher, respectively, than its potency in blocking calcium channels, alpha-adrenoceptors, and histamine receptors. The IC50 values were in the microM range. Compared to bladder muscarinic receptors, the active metabolite, 5-HM, was >900 times less potent at these locations[1].
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ln Vivo |
In vivo tolterodine metabolism was extensive[2]. Tolterodine at 1 or 3 mg/kg did not affect memory in the passive-avoidance test; the percentage of animals crossing and the latency to cross were similar to controls. On the other hand, scopolamine caused a memory impairment, which resulted in a reduction in the latency to cross and an increase in the quantity of animals crossing[3].
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Animal Protocol |
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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. |
Molecular Formula |
C22H31NO.C4H6O6
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Molecular Weight |
475.57
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CAS # |
124937-52-6
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SMILES |
OC1=CC=C(C=C1[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2)C.O=C([C@@H]([C@H](C(O)=O)O)O)O
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InChi Key |
TWHNMSJGYKMTRB-KXYUELECSA-N
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InChi Code |
InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;1-,2-/m11/s1
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Chemical Name |
(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1027 mL | 10.5137 mL | 21.0274 mL | |
5 mM | 0.4205 mL | 2.1027 mL | 4.2055 mL | |
10 mM | 0.2103 mL | 1.0514 mL | 2.1027 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.