Leff P, Dougall I G
Department of Pharmacology, Fisons Research and Development Laboratories, Loughborough, Leics., UK.
Trends Pharmacol Sci. 1993 Apr;14(4):110-2. doi: 10.1016/0165-6147(93)90080-4.
In his article in last month's issue of TiPS (14, 89-91), Douglas Craig discussed the application of the Cheng-Prusoff relationship to the analysis of antagonists in functional experiments. Craig described how the translation of this method from biochemistry to pharmacology can be accompanied by errors due to theoretical misunderstanding. He also emphasized the lower level of rigour associated with this means of estimating antagonist affinity constants compared with Schild analysis. In this article, Paul Leff and Iain Dougall extend Craig's arguments by describing some additional ways in which the application of the Cheng-Prusoff method to pharmacological experiments are likely to result in misinterpretation and erroneous estimates of antagonist affinity.
道格拉斯·克雷格在上个月《药物科学趋势》(第14卷,第89 - 91页)上发表的文章中,讨论了程 - 普鲁索夫关系在功能实验中拮抗剂分析的应用。克雷格描述了这种方法从生物化学转换到药理学的过程中,如何因理论误解而出现错误。他还强调,与希尔德分析相比,这种估计拮抗剂亲和常数的方法严谨性较低。在本文中,保罗·莱夫和伊恩·道高尔扩展了克雷格的观点,描述了程 - 普鲁索夫方法应用于药理实验时,可能导致拮抗剂亲和力误解和错误估计的一些其他情况。