哌啶衍生物作为神经营养药物结构组分的应用前景

A. Vasilyuk, V. Kozlovsky
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引用次数: 1

摘要

哌啶是最常见的杂环化合物之一,其衍生物在许多药理学组中都有发现,包括嗜神经药物。这些化合物在镇痛药中数量众多,除了“经典”的promedol、芬太尼及其衍生物外,本文还介绍了具有镇痛活性和哌啶循环的新化合物的研究结果。对氟哌啶醇和利培酮等哌啶类抗精神病药物的研究已经进行了回顾,并阐明了通过对多巴胺和5 -羟色胺受体的作用而显示出抗精神病活性的新化合物。本文分析了哌醋甲酯对注意缺陷/多动障碍(ADHD)患者大脑影响的数据,有助于了解该疾病中发生的障碍。替加滨被认为是一种抗癫痫药,可以减少部分癫痫的抗性发作次数,并激活小胶质细胞,可能对神经退行性疾病有效。最后一节专门介绍治疗阿尔茨海默病(AD)的药物,即多奈哌齐,其修饰物,以及一些可能通过抑制Aβ42蛋白合成来抑制AD进展的新化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PROMISING DIRECTIONS FOR THE APPLICATION OF PIPERIDINE DERIVATIVES AS STRUCTURAL COMPONENTS OF NEUROTROPIC DRUGS
Piperidine is one of the most common heterocycles, and its derivatives are found in many pharmacological groups, including neurotropic drugs. These compounds are numerous among analgesics, and, in addition to “classical” promedol, fentanyl and its derivatives, the paper presents the results of studying new compounds with analgesic activity and piperidine cycle. Reviews of such piperidine antipsychotics as haloperidol and risperidone have been considered, and new compounds showing antipsychotic activity through their effects on dopamine and serotonin receptors have been elucidated. The data on the influence of methylphenidate on the brain in case of attention deficit/ hyperactivity disorder (ADHD) have been analyzed, which help to understand the disturbances occurring in this disease. Tiagabine has been considered as an antiepileptic agent reducing the number of seizures in resistant forms of partial epilepsy, as well as the activation of microglia and may be effective in neurodegenerative diseases. The last section is devoted to drugs for the treatment of Alzheimer’s disease (AD), namely donepezil, its modifications, and some new compounds potentially capable of inhibiting AD progression through the inhibition of Aβ42 protein synthesis.
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