Calderone V, Martinotti E
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università degli Studi di Pisa, Italy.
J Pharmacol Toxicol Methods. 1998 Nov;40(4):207-10. doi: 10.1016/s1056-8719(99)00007-6.
In functional pharmacology, the Furchgott's analysis and the Waud's analysis are the most widely used among the reliable different methods actually available, for the determination of the dissociation constant of partial agonists. However, they need the application of relatively complicated procedures of manipulation and interpolation of raw data. On the basis of empirical assumptions, this article proposes a new approach, which probably can be considered the simplest method to determine the dissociation constant of a partial agonist, because of the rapid experimental protocol and the easy calculation procedure. Computer-generated concentration-response curves (CRC) for hypothesised partial agonists were analysed by the widely known Waud's analysis and by this new approach. Furthermore, this new analysis was also used to evaluate experimental data from literature, relative to the dissociation constants of alpha-adrenoceptor partial agonists, recorded in rabbit and rat aortae and calculated by the Waud's method. The results obtained by the new approach, both for the computer-generated and for the experimentally studied partial agonists, showed a high level of accuracy, when compared with the classical Waud's analysis.
在功能药理学中，Furchgott分析法和Waud分析法是实际可用的可靠不同方法中应用最广泛的，用于测定部分激动剂的解离常数。然而，它们需要应用相对复杂的原始数据处理和内插程序。基于经验假设，本文提出了一种新方法，由于其实验方案快速且计算程序简便，可能被认为是测定部分激动剂解离常数的最简单方法。通过广为人知的Waud分析法和这种新方法对假设的部分激动剂的计算机生成浓度-反应曲线（CRC）进行了分析。此外，这种新分析方法还用于评估文献中的实验数据，这些数据与α-肾上腺素能受体部分激动剂的解离常数有关，记录于兔和大鼠主动脉，并通过Waud法计算得出。与经典的Waud分析法相比，新方法对计算机生成的和实验研究的部分激动剂所获得的结果都显示出了很高的准确性。
