Vaishnavi S Neil, Nemeroff Charles B, Plott Susan J, Rao Srinivas G, Kranzler Jay, Owens Michael J
Laboratory of Neuropsychopharmacology, Department of Psychiatry and Behavioral Sciences, Emory University, Atlanta, GA 30322, USA.
Biol Psychiatry. 2004 Feb 1;55(3):320-2. doi: 10.1016/j.biopsych.2003.07.006.
Though selective serotonin reuptake inhibitors have revolutionized the field of psychiatry with demonstrated efficacy in affective and anxiety disorders with minimal side effects, norepinephrine-serotonin reuptake inhibitors may provide efficacy similar to tricyclic antidepressants without the adverse side effects associated with tricyclic antidepressants.
The affinity and selectivity of milnacipran, duloxetine, venlafaxine, citalopram, amitriptyline, and nortriptyline were determined for the human serotonin, norepinephrine, and dopamine transporters.
Both milnacipran and duloxetine were potent inhibitors of serotonin and norepinephrine uptake. Unlike duloxetine and venlafaxine, milnacipran appears serotonin transporter selective in binding (ratio = 2.61) and norepinephrine transporter selective in uptake (ratio =.45).
Milnacipran's binding and uptake inhibition profile more closely resembles that of the tricyclic antidepressants than that of duloxetine. Whether these differences observed in vitro manifest themselves in vivo is not clear.
尽管选择性5-羟色胺再摄取抑制剂已彻底改变了精神病学领域，在情感障碍和焦虑症方面疗效显著且副作用极小，但去甲肾上腺素-5-羟色胺再摄取抑制剂可能具有与三环类抗抑郁药相似的疗效，却没有三环类抗抑郁药相关的不良副作用。
测定了米那普明、度洛西汀、文拉法辛、西酞普兰、阿米替林和去甲替林对人5-羟色胺、去甲肾上腺素和多巴胺转运体的亲和力和选择性。
米那普明和度洛西汀都是5-羟色胺和去甲肾上腺素摄取的强效抑制剂。与度洛西汀和文拉法辛不同，米那普明在结合方面似乎对5-羟色胺转运体具有选择性（比率 = 2.61），在摄取方面对去甲肾上腺素转运体具有选择性（比率 = 0.45）。
与度洛西汀相比，米那普明的结合和摄取抑制特征更类似于三环类抗抑郁药。这些体外观察到的差异在体内是否会表现出来尚不清楚。
