论文部分内容阅读
早老性痴呆症患者大脑内的神经递质有着非常相同的变化,胆碱作用性神经细胞有减少的趋势,故对乙酰胆碱酯酶拮抗剂毒扁豆碱及他克林进行了广泛的研究。通过随机筛选发现苄基哌嗪衍生物对大鼠显示出类似胆碱功能药物的作用。用苄基哌啶代替苄基哌嗪部分发现可提高桔抗乙酰胆碱脂酶的活性。即使用酮基代替酰胺基也仍保持活性。因此环酰胺显示出增强桔抗活性作用。据此得到茚满酮衍生物.盐酸多奈哌齐(E2020)较其它化合物各方面效果均优。盐酸多奈哌齐的临床研究获得了较好的结果,美国食品与药品管理局于1996年批准用于早老性痴呆症的冶疗.现已在30多个国家上市。
Neurotransmitters in the brain of patients with Alzheimer’s disease have very similar changes, and cholinergic neurons have a tendency to decrease. Therefore, acetylcholinesterase antagonists physostigmine and tacrine have been extensively studied. Benzylpiperazine derivatives were found to have cholinergic-like effects on rats by random selection. Substituting benzyl piperidine for the benzyl piperazine moiety increased the activity of the anti-acetylcholinesterase. Even with keto groups instead of amide groups still remain active. Cyclic amides thus show an enhancement of the anti-tumor activity of orange. Indanone derivatives are thus obtained. Donepezil hydrochloride (E2020) is superior to other compounds in all aspects. Clinical trials of donepezil hydrochloride have yielded better results and the Food and Drug Administration approved its use in the treatment of Alzheimer’s disease in 1996. Now in more than 30 countries listed.