塔克林
加兰他明
竞争对手
多奈哌齐
胆碱酯酶
美金刚
药理学
阿尔茨海默病
乙酰胆碱酯酶
医学
疾病
痴呆
化学
内科学
生物化学
酶
作者
Jan Korábečný,Katarína Spilovská,Ondřej Benek,Kamil Musílek,Ondřej Soukup,Kamil Kuča
出处
期刊:PubMed
日期:2012-10-01
卷期号:61 (5): 210-21
被引量:1
摘要
Cholinesterase inhibitors have beneficial effects on the cognitive, functional, and behavioural symptoms of Alzheimers disease (AD). Up to date, they represent almost the only drugs approved by the U.S. Food and Drug Administration agency for AD treatment. The group involves donepezil, rivastigmine and galantamine. Apart from the above mentioned cholinesterase inhibitors, memantine is used for AD treatment as well acting as Nmethyl-D-aspartate (NMDA) non-competitive antagonist. Tacrine (9-amino-1,2,3,4-tetrahydroacridine) was the first cholinesterase inhibitor approved for symptomatic AD treatment. However, its several side effects (hepatotoxicity and gastrointestinal discomfort) limited tacrine further use. Recently, novel tacrine analogues are extensively investigated in endeavour to find less toxic compounds with the "multi-target directed ligand" profile affecting more AD pathological mechanisms. The following study summarizes the knowledge of up to date published tacrine analogues, their structural aspects and biological properties. According to structural aspects, tacrine derivatives are divided into three groups, where they are discussed.
科研通智能强力驱动
Strongly Powered by AbleSci AI