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    5-hydroxymethyl tolterodine (PNU 200577)
    5-hydroxymethyl tolterodine (PNU 200577)

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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 #: V1168
    CAS #: 207679-81-0 Purity ≥98%

    Description: 5-hydroxymethyl tolterodine (Desfesoterodine, PNU 200577, PNU-200577, 5HMT, 5HM; 5-HMT, 5-HM), the active metabolite of tolterodine which is a medication used treat overactive bladder, is a novel and potent muscarinic receptor antagonist with a Kb of 0.84 nM. It is a major and pharmacologically active metabolite of tolterodine which used to treat frequent urination, urinary incontinence, or urinary urgency. . 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 

    References: Pharmacol Toxicol. 1997 Oct;81(4):169-72.

    Related CAS #: 380636-50-0 (fumarate)   207679-81-0 (free base)    

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    Molecular Weight (MW)341.49 
    FormulaC22H31NO2 
    CAS No.207679-81-0 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 68 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: 68 mg/mL (199.1 mM)
    Other info

    Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol

    InChi Key: DUXZAXCGJSBGDW-HXUWFJFHSA-N

    InChi Code: InChI=1S/C22H31NO2/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3/t20-/m1/s1

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

    SynonymsDesfesoterodine, PNU-200577; 5-HMT, 5-HM; PNU200577; PNU 200577


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    In Vitro

    In vitro activity: 5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure.

    In Vivo5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. 
    Animal modelMale guinea-pigs 
    Formulation & DosageDissolved in saline; 2 nmol/kg -203 nmol/kg; i.v. injection
    References

    Pharmacol Toxicol. 1997 Oct;81(4):169-72. 


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

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