Home Neuronal Signaling 5-HT Receptor inhibitor - Serotonin Transporter inhibitor Dapoxetine HCl For research use only.

Dapoxetine HCl

Synonyms: LY-210448

Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

Dapoxetine HCl Chemical Structure

Dapoxetine HCl Chemical Structure

CAS: 129938-20-1

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Biological Activity

Description Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
Targets
5-HT [1]
In vitro
In vitro 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. [1] 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. [2] 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. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03018743 Unknown status Premature Ejaculation Pusan National University Hospital January 2017 --
NCT01928563 Unknown status Healthy Male Subjects Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. September 2013 Phase 1
NCT01366664 Completed Ejaculation Janssen Research & Development LLC April 2011 Phase 1
NCT01063881 Completed Sexual Dysfunction Physiological Johnson & Johnson Pte Ltd May 2010 Phase 3
NCT00211094 Completed Ejaculation Alza Corporation DE USA Phase 3

Chemical lnformation & Solubility

Molecular Weight 341.87 Formula

C21H23NO.HCl
CAS No. 129938-20-1 SDF Download Dapoxetine HCl SDF
Smiles CN(C)C(CCOC1=CC=CC2=CC=CC=C21)C3=CC=CC=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (198.9 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 68 mg/mL

Ethanol : 68 mg/mL


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In vivo
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