Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE)[1].
In Vitro, Dapoxetine binds to 5-HT, norepinephrine, and dopamine reuptake transporters and inhibits 5-HT, norepinephrine, and dopamine uptake with an order of potency: 5-HT >norepinephrine≫dopamine.
Dapoxetine inhibits the uptake of [3H]5-HT by the 5-HT reuptake transporter with a value of 1.12 nM, and Dapoxetine inhibits the uptake of [3H]norepinephrine into cells utilizing the norepinephrine reuptake transporter and uptake of [3H]dopamine by the dopamine reuptake transporter with IC50 values of 202 nM and 1720 nM, respectively[1].
In Vivo, Dapoxetine (oral gavage; 1-10 mg/kg; once daily) significantly inhibits testosterone mediated increase in the prostate weight and relative prostate weight and attenuates testosterone-induced prostatic hyperplasia in rats[2].
References:
[1]. Muammer Kendirci, et al. Dapoxetine, a novel selective serotonin transport inhibitor for the treatment of premature ejaculation. Ther Clin Risk Manag. 2007 Jun;3(2):277-89.
[2]. Rabab H Sayed, et al. Dapoxetine attenuates testosterone-induced prostatic hyperplasia in rats by the regulation of inflammatory and apoptotic proteins. Toxicol Appl Pharmacol. 2016 Nov 15;311:52-60.