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.
Dapoxetine (LY-210448) 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 可用于早泄 (PE) 的相关研究。
在体外，达泊西汀与 5-HT、去甲肾上腺素和多巴胺再摄取转运体结合，并抑制 5-HT、去甲肾上腺素和多巴胺的摄取，其效力顺序为：5-HT >去甲肾上腺素≫多巴胺。
达泊西汀抑制 5-HT 再摄取转运体对 [3H]5-HT 的摄取，其 IC50 值为 1.12 nM；达泊西汀抑制细胞利用去甲肾上腺素再摄取转运体对 [3H]去甲肾上腺素的摄取，抑制多巴胺再摄取转运体对 [3H]多巴胺的摄取，其 IC50 值分别为 202 nM 和 1720 nM[1]。
在体内，达泊西汀（口服管饲；1-10毫克/千克；每日一次）显著抑制睾酮介导的前列腺重量和相对前列腺重量的增加，并减轻大鼠睾酮诱导的前列腺增生[2]。