Neurotransmitter transporters: fruitful targets for CNS drug discovery
Neurotransmitter transporters: fruitful targets for CNS drug discovery
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DOI：
10.1038/sj.mp.4000728
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发表时间：
2000-07-01
影响因子：
11
通讯作者：
Iversen, L
中科院分区：
文献类型：
--
作者：
Iversen, L
在神经递质转运家族中已经确定了20多个成员。其中包括单胺类和氨基酸类神经递质的细胞表面再摄取机制，以及参与神经递质储存的囊泡转运机制。去甲肾上腺素和血清素再摄取转运体是抗抑郁药物的关键靶点。临床有效的抗抑郁药包括选择性摄取NE或5 -羟色胺的药物，以及混合作用的化合物。多巴胺转运体在介导可卡因和安非他明的作用以及赋予多巴胺神经毒素选择性方面起着关键作用。迄今为止，在氨基酸转运体研究中唯一临床使用的化合物是抗癫痫药物替加滨，一种GABA摄取抑制剂。
More than 20 members have been identified in the neurotransmitter transporter family. These include the cell surface re-uptake mechanisms for monoamine and amino acid neurotransmitters and vesicular transporter mechanisms involved in neurotransmitter storage. The norepinephrine and serotonin re-uptake transporters are key targets for antidepressant drugs. Clinically effective antidepressants include those with selectivity for either NE or serotonin uptake, and compounds with mixed actions. The dopamine transporter plays a key role in mediating the actions of cocaine and the amphetamines and in conferring selectivity on dopamine neurotoxins. The only clinically used compound to come so far from research on amino acid transporters is the antiepileptic drug tiagabine, a GABA uptake inhibitor.