University of Defense, Faculty of Military Health Sciences, Trebesska 1575, 50001 Hradec Kralove, Czech Republic.
Expert Opin Ther Pat. 2012 Aug;22(8):871-86. doi: 10.1517/13543776.2012.701620. Epub 2012 Jul 6.
Both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are present in the body in large amounts. AChE is an important part of the cholinergic nervous system taking place in the central and peripheral nervous system. AChE is a target of several toxins such as insecticide carbofuran, nerve agents, sarin, soman, tabun and VX. Beside toxins, drugs for treatment of Alzheimer's disease and myasthenia gravis, such as galantamine, donepezil, rivastigmine, tacrine, huperzine, pyridostigmine and neostigmine, are known.
The review gives an overview of the importance of the cholinergic nervous system, the biochemistry of AChE and the role of AChE inhibitors. Current efforts to introduce potent drugs for Alzheimer's disease therapy and reduce toxicity, while keeping the maximal pharmacological effect, are also discussed.
The current research effort into AChE inhibitors can be divided into two categories. First, new toxins useful for agricultural purposes and second, novel drugs that need to be prepared, although there is less interest in the new toxins. The research for drugs for Alzheimer's disease needs to focus on inhibitors that reduce the deposition of amyloid plaques, but do not initiate AChE expression.
乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）在体内大量存在。AChE 是胆碱能神经系统的重要组成部分，存在于中枢和周围神经系统中。AChE 是几种毒素的靶标，如杀虫剂呋喃丹、神经毒剂沙林、梭曼、塔崩和 VX。除了毒素，用于治疗阿尔茨海默病和重症肌无力的药物，如加兰他敏、多奈哌齐、利斯的明、他克林、石杉碱甲、吡斯的明和新斯的明，也是已知的。
综述概述了胆碱能神经系统的重要性、AChE 的生物化学以及 AChE 抑制剂的作用。还讨论了目前为引入治疗阿尔茨海默病的有效药物和降低毒性而同时保持最大药理作用所做的努力。
目前对 AChE 抑制剂的研究可分为两类。第一类是用于农业目的的新型毒素，第二类是需要制备的新型药物，尽管对新型毒素的兴趣较小。用于治疗阿尔茨海默病的药物研究需要集中于能减少淀粉样斑块沉积而不引发 AChE 表达的抑制剂。
