摘要
背景:吉氏甲醚(Gm)是钩藤中吲哚生物碱之一,是尤库坎的有效成分,能改善精神错乱的行为和心理症状。a(Bpsd)在几种类型的痴呆症患者。GM的药理作用与5-羟色胺(5-HT)受体亚型有关. 目的:利用我们自己的数据和前人的研究成果,对GM与脑内5-HT受体亚型的结合特性进行综述。 方法:对几种5-羟色胺受体亚型进行竞争性受体结合和激动剂/拮抗剂活性测定。此外,本文还描述了药物动力学和脑分布。在PubMed上搜索了GM的基因。 结果:GM与5-HT1A、5-HT1B、5-HT2A、5-HT2B、5-HT2C、5-HT4、5-HT5A、5-HT6、5-HT7等5-HT受体亚型结合.。在这些受体中,gm对5-hT1A Re具有部分激动剂活性。5-HT2A、5-HT2B、5-HT2C和5-HT7受体的受体及其拮抗活性。此外,GM还被各种CYP亚型代谢,主要是CYP3A4。在血液中检测到亲本/未改变的gm基因。大鼠口服YKS后的ND脑。在大脑中,gm主要与神经元样大细胞上的5-HT1A、5-HT2A、5-HT2B、5-HT2C和5-HT7受体结合,主要在额叶皮质。[医] 十分之一效度(顺势疗法),金伯克氏X线剂量单位 结论:GM是一种具有重要药理作用的生物碱,通过与多种5-HT受体亚型结合,调节多种5-羟色胺的活性或功能。因此,回顾了最近的5-HT受体相关的证据表明转基因对YKS药理作用的部分原因。
关键词: 葛根素甲醚,5-羟色胺受体,药动学,药理学方面,尤库桑,BPSD,痴呆。
Current Medicinal Chemistry
Title:Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook
Volume: 25 Issue: 9
关键词: 葛根素甲醚,5-羟色胺受体,药动学,药理学方面,尤库桑,BPSD,痴呆。
摘要: Background: Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes.
Objective: The aim of this article is to review the binding characteristics of GM to the 5-HT receptor subtypes in the brains using our own data and previous findings.
Method: Competitive receptor-binding and agonist/antagonist activity assays for several 5-HT receptor subtypes were performed. Moreover, the articles describing pharmacokinetics and brain distribution of GM were searched in PubMed.
Results: GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5- HT4, 5-HT5A, 5-HT6, and 5-HT7. Among these receptors, GM had partial agonistic activity for 5-HT1A receptors and antagonistic activity for 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors. Also, GM was metabolized by various CYP isoforms, mainly CYP3A4. Parent/unchanged GM was detected in both the blood and brain of rats after oral administration of YKS. In the brains, GM was presumed to bind to 5- HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors on neuron-like large cells mainly in the frontal cortex.
Conclusion: These results suggest that GM is a pharmacologically important alkaloid that regulates various serotonergic activities or functions by binding to multiple 5-HT receptor subtypes. Thus, this review provides recent 5-HT receptor-related evidence that GM is partly responsible for pharmacological effects of YKS.
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Cite this article as:
Serotonin Receptor Binding Characteristics of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, Current Medicinal Chemistry 2018; 25 (9) . https://dx.doi.org/10.2174/0929867324666170320114713
DOI https://dx.doi.org/10.2174/0929867324666170320114713 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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