腺苷A2A拮抗剂在帕金森病中的作用和进展

W. Aryati, Nabilah Nurtika Salamah, Rezi Riadhi Syahdi, Arry Yanuar
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引用次数: 1

摘要

腺苷是一种神经调节剂,调节身体对多巴胺的反应,多巴胺是大脑中负责运动、情感、学习和记忆功能的另一种神经递质。腺苷是一种g蛋白偶联受体,有四种亚型,分别是a1、2A、2B和a3。腺苷a2a位于大脑纹状体中。拮抗剂干扰GABA的释放,调节乙酰胆碱,释放多巴胺,促进多巴胺受体的信号传递。因此,它可以减轻帕金森病的运动症状。腺苷a2a拮抗剂也被认为具有神经保护作用。一些化合物作为选择性腺苷a2a拮抗剂已被报道并进行了临床试验,包括iststradefylline、preladenant、tozadenant、vipadenant、ST-1535和SYN-115。来自天然化合物的非选择性腺苷a2a拮抗剂是咖啡因和茶碱。,
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The Role and Development of the Antagonist of Adenosine A2A in Parkinson’s Disease
Adenosine is a neuromodulator that regulates the body’s response to dopamine and another neurotransmitter in the brain that is responsible for motoric, emotion, learning, and memory function. Adenosine is a G-protein-coupled receptor and has four subtypes, which are A 1, A 2A , A 2B , and A 3 . Adenosine A 2A is located in the striatum of the brain. Antagonist interferes with GABA releasing, modulates acetyl-choline and releases dopamine, and also facilitates dopamine receptor’s signaling. Therefore, it can reduce motoric symptoms in Parkinson’s disease. Adenosine A 2A antagonist is also believed to have neuroprotective effects. Several compounds have been reported and have undergone clinical test as selective adenosine A 2A antagonists, including istradefylline, preladenant, tozadenant, vipadenant, ST-1535, and SYN-115. Nonselective adenosine A 2A antagonists from natural compounds are caffeine and theophylline. ,
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