The Hill equation and the origin of quantitative pharmacology
The Hill equation and the origin of quantitative pharmacology
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DOI：
10.1007/s00407-012-0098-5
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发表时间：
2012-07-01
影响因子：
0.5
通讯作者：
Tosaki, Arpad
中科院分区：
文献类型：
--
作者：
Gesztelyi, Rudolf;Zsuga, Judit;Tosaki, Arpad
本文回顾了已有100年历史的Hill方程（发表于1910年1月22日），这是第一个将可逆关联的结果（例如，复合物的浓度，效应的大小）与其中一种相关物质的可变浓度（另一种物质以恒定且相对较低的浓度存在）联系起来的公式。此外，Hill方程是药理学中第一个（也是最简单的）定量受体模型。虽然Hill方程是一个经验受体模型（其参数仅具有简单配体结合反应的物理化学意义），但它只需要对所研究的激动剂的作用机制有少量的先验知识，就可以可靠地拟合浓度-响应曲线数据并产生有用的结果（与大多数先进的受体模型相反）。因此，Hill方程仍然是包括药物发现在内的生理和药理学研究的重要工具，并且是开发新的药理学模型的理论基础。
This review addresses the 100-year-old Hill equation (published in January 22, 1910), the first formula relating the result of a reversible association (e.g., concentration of a complex, magnitude of an effect) to the variable concentration of one of the associating substances (the other being present in a constant and relatively low concentration). In addition, the Hill equation was the first (and is the simplest) quantitative receptor model in pharmacology. Although the Hill equation is an empirical receptor model (its parameters have only physico-chemical meaning for a simple ligand binding reaction), it requires only minor a priori knowledge about the mechanism of action for the investigated agonist to reliably fit concentration-response curve data and to yield useful results (in contrast to most of the advanced receptor models). Thus, the Hill equation has remained an important tool for physiological and pharmacological investigations including drug discovery, moreover it serves as a theoretical basis for the development of new pharmacological models.