摘要
多巴胺受体激动剂的使用是治疗帕金森氏病和相关的中枢神经系统(CNS)神经退行性疾病的关键。尽管有一些商业化的多巴胺受体激动剂目前被成功地应用在疾病的最初阶段,但是他们往往以来由于副作用不能长期提供持续的临床效果,如增生物,嗜睡,恶心,低血压,除此以外还有强迫行为等。现在正在开发副作用少的新的多巴胺受体激动剂。当疾病的进展和患者没有响应标准的多巴胺能治疗或副作用增加时,这些新的化合物提供了一种替代物。化学,特别是化学合成,在合成多巴胺受体激动剂到临床发挥了重要作用,并继续在减少不必要的副作用的长期治疗发展新的和必要的药物中至关重要。大量的母体化合物的结构修饰不仅导致增强激动并且部分激动剂或对一个或更多的多巴胺受体起拮抗作用。在某些情况下,这些活动都伴随着激动剂作用于5-羟色胺受体,表明在治疗精神分裂症多巴胺能药物的临床应用潜力。本文总结了多巴胺能药物化学合成,他们的亲和力以及将凸显相应的激动/拮抗剂作用。
关键词: 多巴胺,多巴胺受体激动剂,多巴胺受体,帕金森病,不对称合成,阿朴吗啡。
Current Medicinal Chemistry
Title:Design and Synthesis of Dopaminergic Agonists
Volume: 23 Issue: 25
Author(s): Maria Soledad Matute, Rosa Matute, Pedro Merino
Affiliation:
关键词: 多巴胺,多巴胺受体激动剂,多巴胺受体,帕金森病,不对称合成,阿朴吗啡。
摘要: The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to provide sustained clinical benefit for a long period due to the appearance of side-effects such as augmentation, sleepiness, nausea, hypothension, and compulsive behaviors among others. New dopaminergic agonists with less side effects are being developed. These novel compounds offer an alternative when the disease progresses and patients fail to respond to standard dopaminergic treatments or side-effects increased. Chemistry, and in particular chemical synthesis, has played a major role in bringing synthetic dopaminergic agonists to the clinic and continues to be crucial for the development of new and necessary drugs for long-term treatments with less undesired side effects. A number of structural modifications of parent compounds have led to enhanced agonism but also partial agonism or even antagonism of one or more dopamine receptors. In some cases, these activities are accompanied by agonist effect at serotonin receptors which suggests a potential clinical application in the treatment of schizophrenia In this review, chemical synthesis of dopaminergic agents, their affinity, and the corresponding agonist/antagonist effects will be highlighted.
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Cite this article as:
Maria Soledad Matute, Rosa Matute, Pedro Merino , Design and Synthesis of Dopaminergic Agonists, Current Medicinal Chemistry 2016; 23 (25) . https://dx.doi.org/10.2174/0929867323666160504103621
DOI https://dx.doi.org/10.2174/0929867323666160504103621 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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