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 No. 129938-20-1

Purity & Quality Control

Dapoxetine HCl Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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 Information & 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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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