靶点

norepinephrine (NE) transporter

IC50

5 nM (Ki)

体外研究

Atomoxetine is a selective norepinephrine reuptake inhibitor with Ki of 5 nM, compared with 77 and 1451 nM for binding to serotonin and dopamine transporters.

体内研究

In microdialysis studies, atomoxetine increases extracellular (EX) levels of NE in prefrontal cortex (PFC) 3-fold, but does not alter 5-HTEX levels. Atomoxetine also increases DAEX concentrations in PFC 3-fold, but does not alter DAEX in striatum or nucleus accumbens. Atomoxetine increases Fos by 3.7-fold in PFC, but not in the striatum or nucleus accumbens. Atomoxetine selectively inhibits the presynaptic uptake of norepinephrine in adrenergic neurons in animals, and has activity in animal models of depression.

溶解性

DMSO 58 mg/mL，水 2 mg/mL，乙醇 37 mg/mL

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO