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    Tolterodine tartrate (Kabi-2234; PNU-200583E)
    Tolterodine tartrate (Kabi-2234; PNU-200583E)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1161
    CAS #: 124937-52-6Purity ≥98%

    Description: 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. 

    References: Eur J Pharmacol. 1997 May 30;327(2-3):195-207; J Urol. 2007 Jul;178(1):326-31

    Related CAS #: 124937-51-5 (free base)   124937-52-6 (tartrate)    

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    Molecular Weight (MW)475.57
    FormulaC22H31NO.C4H6O6
    CAS No.124937-52-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 95 mg/mL (199.8 mM)
    Water: 17 mg/mL (35.7 mM)
    Ethanol: 6 mg/mL (12.6 mM)
    Other info

    Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate

    InChi Key: TWHNMSJGYKMTRB-KXYUELECSA-N

    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

    SMILES Code: OC1=CC=C(C)C=C1[[email protected]@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O

    SynonymsPNU-200583 E; PNU200583E; Tolterodine tartrate; PNU-200583E; PNU 200583E; Detrol LA; Detrusitol.


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    In Vitro

    In vitro activity: Tolterodine has a high affinity and specificity for muscarinic receptors in vitro and it exhibits selectivity for the urinary bladder over salivary glands in vivo. Tolterodine is a new muscarinic receptor antagonist intended for the treatment of urinary urge incontinence and other symptoms related to an overactive bladder. Tolterodine effectively inhibits carbachol-induced contractions of isolated strips of urinary bladder from guinea pigs in a concentration-dependent, competitive manner. Tolterodine binds with high affinity to muscarinic receptors in urinary bladder (Ki 2.7 nM), heart (Ki 1.6 nM), cerebral cortex (Ki 0.75 nM) and parotid gland (Ki 4.8 nM) from guinea pigs and in urinary bladder from humans (Ki 3.3 nM).

    In VivoTolterodine (1 mg/kg, i.v.) is significantly more potent in inhibiting acetylcholine-induced urinary bladder contraction than electrically-induced salivation in the anaesthetised cat. Tolterodine administered intravenously increases the mean micturition interval, bladder capacity and micturition volume in normal rats and resiniferatoxin treated rats. Tolterodine (2 nM/kg) significantly increases bladder capacity (BC) in saline vehicle- cerebral infarct rats without increasing residual volume but it has no effects on BC in resiniferatoxin- cerebral infarct rats. Tolterodine tartrate (0.1 and 1.0 mg/kg) significantly decreases the number and amplitude of non-voiding contractions by 38-74% and 29-44%, respectively, and increases bladder capacity by 19-51% in female rats with bladder outlet obstruction.
    Animal modelCat
    Formulation & Dosage1 mg/kg, i.v.
    References

    Eur J Pharmacol. 1997 May 30;327(2-3):195-207; J Urol. 2007 Jul;178(1):326-31.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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