Dasotraline hydrochloride 是具有阻断多巴胺 (IC50=4 nM)，去甲肾上腺素 (IC50=6 nM) 和三羟色胺转运蛋白 (IC50=11 nM)的三重再摄取抑制剂。

Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that inhibits dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

Acute administration of dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α2, D2 and 5-HT1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. SEP-225289 is equipotent at inhibiting 5-HT and NE transporters because it prolongs to the same extent the time required for a 50% recovery of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE[1]. Average dopamine and serotonin transporter occupancies increase with increasing doses of SEP-225289. Average dopamine and serotonin transporter occupancies are 33%±11% and 2%±13%, respectively, for 8 mg; 44%±4% and 9%±10%, respectively, for 12 mg; and 49%±7% and 14%±15%, respectively, for 16 mg[2].

675126-08-6

C16H16Cl3N

328.66

达索曲林盐酸盐;SEP-225289 hydrochloride

DMSO:31 mg/mL (94.32 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years