可视化抗抑郁药物的药理活性:一种新方法

H. J. Derijks, E. Heerdink, R. Janknegt, F. H. P. Koning, B. Olivier, A. Loonen, A. Egberts
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引用次数: 26

摘要

抗抑郁药具有不同的受体结合谱,这与治疗作用和药物不良反应有关。我们构建了一个模型,根据抗抑郁药与大多数常见转运体和受体位点的结合特性对其进行分类。通过计算5-HT(5-羟色胺)再摄取转运体、去甲肾上腺素再摄取转运体、5- ht2c受体、m3受体、h1受体和1-受体的受体占用率来量化受体结合。采用层次聚类分析(HCA)和主成分分析(PCA)对不同受体占有相似模式的抗抑郁药进行分类。此外,为了可视化(a)抗抑郁药结合谱之间的对称性,构建了雷达图。在这两种分析的基础上,确定了四类具有相似药理特性的抗抑郁药。该模型可能在医疗实践中成为一种有用的工具,并可作为进入市场的药物不良反应的预测模型。
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Visualizing pharmacological activities of antidepressants: A novel approach
Antidepressants have different receptor binding profiles, which are related to therapeutic action and adverse drug reactions. We constructed a model to classify antidepressants on the basis of their binding properties of most common transporter- and receptor sites. Receptor binding was quantified by calculating receptor occupancy for the 5-HT (serotonin) reuptake transporter, norepinephrinic reuptake transporter, 5-HT2C-receptor, M3-receptor, H1-receptor and 1- receptor. To identify groups of antidepressants that show similar patterns of receptor occupancy for different receptors, hierarchical cluster analysis (HCA) and principle component analysis (PCA) were used. In addition, to visualize (a)symmetry between binding profiles of antidepressants, radar plots were constructed. On the basis of both analyses, four clusters of antidepressants which exert similar pharmacological properties were identified. Potentially, this model could be a helpful tool in medical practice and may be used as a prediction model for adverse effects of drugs entering the market.
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