Dapoxetine (LY-210448) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine hydrochloride can be used for the research of premature ejaculation (PE).
性状
Solid
IC50 & Target[1][2]
Target: serotonin reuptake
体外研究(In Vitro)
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 [H]5-HT by the 5-HT reuptake transporter with a value of 1.12 nM, and Dapoxetine inhibits the uptake of [H]norepinephrine into cells utilizing the norepinephrine reuptake transporter and uptake of [H]dopamine by the dopamine reuptake transporter with IC50 values of 202 nM and 1720 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: H2O : 100 mg/mL (292.51 mM; Need ultrasonic)DMSO : ≥ 32 mg/mL (93.60 mM)