2S)-N-[N-(3,5-二氟苯乙酰基)-L-丙氨酰]-2-苯基甘氨酸叔丁酯

Dapoxetine (LY-210448) hydrochloride 是一种具有口服活性的选择性血清素再摄取 (serotonin reuptake) 抑制剂 (SSRI)。Dapoxetine hydrochloride 可用于早泄 (PE) 的相关研究。

Dapoxetine hydrochloride 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 hydrochloride 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]

Dapoxetine hydrochloride (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].