Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

GRK2:14 μM

Paroxetine在ED50 1-3 mg/kg PO）可防止对氯苯丙胺（PCA）在大鼠脑中的5-HT消耗作用,表明体内5-HT摄取受阻.Paroxetine对离体大鼠下丘脑突触体产生剂量相关的[3H] -5-HT摄取抑制（ED50 = 1.9 mg/kg）,对[3H] -l-去甲肾上腺素（NA）摄取影响很小（ED50大于30 mg/kg）.

1-300 μM Paroxetine导致ACSF超融合脑干切片中DRN血清素能神经元放电速率浓度依赖性降低,IC50值为1.4 μM。Paroxetine是地昔帕明羟基化的高度有效的抑制剂,抑制常数（Ki）为2 mM,表明其抑制效力比氟西汀或诺氟西汀更强。Paroxetine在大鼠皮层和体外下丘脑突触中,是一种[3H]-5-羟色胺（5-HT）的有效的（Ki=1.1 nM）和特异性抑制剂。Paroxetine显然通过增加细胞外区室中5-HT的浓度来发挥其抗抑郁活性,由此增强血清素能神经传递。 Paroxetine通过形成代谢物中间体复合物来灭活CYP2D6。

Paroxetine is dissolved in DMSO. Cell viability is determined by the tetrazolium salt 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. BV2 and primary microglial cells are initially seeded into 96-well plates at a density of 1×104 cells/well and 5×104 cells/well, respectively. Following treatment, MTT (5 mg/mL in PBS) is added to each well and incubated at 37°C for four hours. The resulting formazan crystals are dissolved in dimethylsulfoxide (DMSO). The optical density is measured at 570 nm, and results are expressed as a percentage of surviving cells compared with the control.