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    Darifenacin HBr (UK88525)
    Darifenacin HBr (UK88525)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1171
    CAS #: 133099-07-7Purity ≥98%

    Description: Darifenacin HBr (formerly known as UK-88525; Emselex; Enablex), the hydrobromide salt of Darifenacin, is a approved medication used to treat urinary incontinence and overactive bladder. It acts as a selective M3 muscarinic receptor antagonist with pKi of 8.9. Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. 

    References: Br J Pharmacol. 1997 Apr;120(8):1409-18; Neurourol Urodyn. 2011 Nov;30(8):1633-8.

    Related CAS #: 133099-04-4 (free base)   133099-07-7 (HBr)    

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    Molecular Weight (MW)507.46 
    FormulaC28H30N2O2.HBr 
    CAS No.133099-07-7 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 117 mg/mL (230.5 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide hydrobromide

    InChi Key: UQAVIASOPREUIT-VQIWEWKSSA-N

    InChi Code: InChI=1S/C28H30N2O2.BrH/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26;/h1-12,19,25H,13-18,20H2,(H2,29,31);1H/t25-;/m1./s1

    SMILES Code: O=C(N)C(C1=CC=CC=C1)([[email protected]]2CN(CCC3=CC4=C(OCC4)C=C3)CC2)C5=CC=CC=C5.[H]Br

    SynonymsUK-88525; Darifenacin; Emselex; Enablex. UK 88525; UK88525; Darifenacin HBr


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    In Vitro

    In vitro activity: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6.

    In VivoDarifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB).  
    Animal modelRats
    Formulation & Dosage0.1 mg/kg i.v.
    References

    Br J Pharmacol. 1997 Apr;120(8):1409-18; Neurourol Urodyn. 2011 Nov;30(8):1633-8. 


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

    Darifenacin HBr
    Effects of (a) methoctramine and (b) darifenacin on the re-contractile concentration-effect curve to (+)-cis-dioxolane obtained after elevation of adenylyl cyclase activity following preferential alkylation of M3 muscarinic receptors. Br J Pharmacol. 1997 Apr;120(8):1409-18.
     
    Darifenacin HBr
    Effects of muscarinic receptor antagonists on (a) amplitude of volume-induced bladder contractions (VIBCAMP) (b) mean arterial pressure in urethane anaesthetized rats. Br J Pharmacol. 1997 Apr;120(8):1409-18.
     
    Darifenacin HBr
    Effect of propranolol (1 mg kg−1, i.v.) on the inhibitory effects of (a) methoctramine and (b) darifenacin on amplitude of volume-induced bladder contractions (VIBCAMP) in urethane anaesthetized rats. Br J Pharmacol. 1997 Apr;120(8):1409-18.


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