product name Dapoxetine HCl
Description: Dapoxetine HCl (also known as LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, 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.
341.87
Formula
C21H23NO.HCl
CAS No.
129938-20-1
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)
Solubility (In vivo)
Synonyms
LY-210448
other peoduct :
| 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Neuropharmacology. 2012 Jun;62(7):2261-6; Naunyn Schmiedebergs Arch Pharmacol. 2012 Jul;385(7):707-16. |
