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多巴胺在中枢神经系统中是一个非常重要的神经递质。在病理生理学上,大脑多巴胺系统涉及多种神经性疾病,包括:帕金森综合症、精神分裂症、躁狂症、抑郁症、毒品成瘾和饮食混乱等。它的作用主要是通过多巴胺受体的五个亚型(D1～D5)进行调节的。药物化学和神经药理学上对多巴胺D1受体和D2受体的研究已经取得了很大的进展,开发出了一系列具有D1、D2受体选择性的配体及药物;然而开发新型的D3、D4、D5受体选择性配体及药物仍然是一个很大的挑战。本文主要讨论多巴胺受体5种亚型的配体研究进展。
Dopamine is a very important neurotransmitter in the central nervous system. In the pathophysiology, the brain dopamine system involves a variety of neurological disorders, including Parkinson’s disease, schizophrenia, mania, depression, drug addiction and diet disorders. Its role is mainly through the five subtypes of dopamine receptors (D1 ~ D5) to regulate. Much progress has been made in the research of medicinal chemistry and neuropharmacology on dopamine D1 receptor and D2 receptor, and a series of ligands and drugs with D1 and D2 receptor selectivity have been developed. However, a new type of D3 , D4, D5 receptor selective ligands and drugs remains a big challenge. This article mainly discusses the research progress of ligands of five subtypes of dopamine receptors.