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    Dapoxetine HCl (LY-210448 HCl)
    Dapoxetine HCl (LY-210448 HCl)

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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 #: V0977
    CAS #: 129938-20-1Purity ≥98%

    Description: Dapoxetine HCl (formerly known as LY210448; LY-210448; trade name Priligy), an antidepressant, is a novel, potent, short-acting and selective serotonin reuptake inhibitor (SSRI) that has alto been used for the treatment of premature ejaculation. It is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Granisetron blocks the delayed rectifier current (IK) of feline isolated ventricular myocytes with a KD of 4.3 mM. Granisetron shows an intrinsic voltage-dependence as the block increases with depolarization. 

    References: Neuropharmacology. 2012 Jun;62(7):2261-6; Naunyn Schmiedebergs Arch Pharmacol. 2012 Jul;385(7):707-16.

    Related CAS: 119356-77-3 (free base) 

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    Molecular Weight (MW)341.87
    FormulaC21H23NO.HCl 
    CAS No.129938-20-1  (HCl); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 68 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: 68 mg/mL (198.9 mM) 
    SMILES CodeCN(C)[[email protected]@H](CCOC1=C2C=CC=CC2=CC=C1)C3=CC=CC=C3.[H]Cl
    SynonymsLY-210448; Dapoxetine HCl; LY 210448; LY210448; Priligy


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    In Vitro

    In vitro activity: Dapoxetine not only reduces the peak amplitude of Kv4.3 currents but also accelerates the decay rate of current inactivation in a concentration-dependent manner. Dapoxetine decreases the integral of the Kv4.3 currents over the duration of a depolarizing pulse with an IC50 of 5.3 μM. Dapoxetine also causes a substantial acceleration in closed-state inactivation. Dapoxetine produces a significant use-dependent block, which is accompanied by a delayed recovery from inactivation of Kv4.3 currents. Dapoxetine decreases the peak amplitude of Kv1.5 currents and accelerates the decay rate of current inactivation in a concentration-dependent manner with an IC50 of 11.6 μM. Dapoxetine decreases the tail current amplitude and slows the deactivation process of Kv1.5, which results in a tail crossover phenomenon. Dapoxetine produces a use-dependent block of Kv1.5 at frequencies of 1 and 2 Hz and slowed the time course for recovery of inactivation. Dapoxetine also appears to be a useful adjunct to morphine, lowering the threshold for analgesia, although Dapoxetine itself has negligible analgesic activity. Dapoxetine is the D-enantiomer of LY 243917 and is 3.5 times more potent as a serotonin reuptake inhibitor than the L-enantiomer.

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    ReferencesNeuropharmacology. 2012 Jun;62(7):2261-6; Naunyn Schmiedebergs Arch Pharmacol. 2012 Jul;385(7):707-16.


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

     

    Dapoxetine HCl

    Neuropharmacology. 2012 Jun;62(7):2261-6.
     

    Dapoxetine HCl

    Neuropharmacology. 2012 Jun;62(7):2261-6.


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