Sasa M
Department of Pharmacology, Hiroshima University School of Medicine.
Nihon Rinsho. 2001 Aug;59(8):1457-64.
Monoamine transporters include plasma membrane and vesicular monoamine transporters(VMAT). The former selectively and Na+/Cl(-)-dependently transport dopamine, noradrenaline and serotonin into the cytoplasma, and the latter non-selectively carries monoamine into the vesicle. These transporters are composed of amino acid groups containing 12 folds more transmembrane components. Cytoplasmic transporters are a target site of certain drugs. Antiepileptic drugs such as SSRI and tricyclic antidepressants bind with serotonin transporter(SERT), noradrenaline transporter(NET) and/or dopamine transporters(DAT) to inhibit transport of monoamines into the cytoplasma, thereby increasing monoamine levels within the synaptic cleft. However, amphetamine, known to induce drug dependence, is transported by DAT and inhibit VMAT to induce reverse-transport of monoamines into the synaptic area, thereby producing psychiatric and behavioral alterations. Thus, monoamine transporters are target sites of drugs, and functional changes in the transporters may be involved in the pathogenesis of affective diseases, schizophrenia and/or personality disorders including neurogenerative diseases such as Parkinson's disease.
单胺转运体包括质膜单胺转运体和囊泡单胺转运体（VMAT）。前者选择性地且依赖Na+/Cl(-)将多巴胺、去甲肾上腺素和5-羟色胺转运到细胞质中，而后者非选择性地将单胺转运到囊泡中。这些转运体由含有12个以上跨膜成分的氨基酸基团组成。细胞质转运体是某些药物的作用靶点。抗癫痫药物如选择性5-羟色胺再摄取抑制剂（SSRI）和三环类抗抑郁药与5-羟色胺转运体（SERT）、去甲肾上腺素转运体（NET）和/或多巴胺转运体（DAT）结合，抑制单胺转运到细胞质中，从而增加突触间隙内的单胺水平。然而，已知会导致药物依赖的苯丙胺通过DAT转运并抑制VMAT，从而诱导单胺逆向转运到突触区域，进而产生精神和行为改变。因此，单胺转运体是药物的作用靶点，转运体的功能变化可能与情感性疾病、精神分裂症和/或人格障碍（包括帕金森病等神经退行性疾病）的发病机制有关。
