Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Dopamine transporter:1451 nM(Ki), 5-HT:77 nM(Ki), NET:5 nM(Ki)

在动物中,Atomoxetine选择性抑制肾上腺素能神经元突触前对去甲肾上腺素的摄取,且对抑郁的动物模型也有活性.在微透析研究中,Atomoxetine对5-HTEX水平无影响,但使前额皮质中细胞外去甲肾上腺素水平升高了3倍.Atomoxetine不改变伏隔核和纹状体中的DAEX和Fos,但会使PFC中DAEX浓度增加3倍、Fos增加3.7倍.

Atomoxetine是去甲肾上腺素重摄取的选择性抑制剂（Ki：5 nM）,而对5-羟色胺（Ki：77 nM）和多巴胺转运蛋白（Ki：1451 nM）的选择性相对较低。