Kenakin T
Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.
Trends Pharmacol Sci. 1995 Jun;16(6):188-92. doi: 10.1016/s0165-6147(00)89020-3.
The description of drug effects on receptor proteins is based on models and equations used to describe mass-action kinetics of molecules and inert surfaces. These models provide an adequate description of drug affinity, that is, how well a molecule binds to a receptor protein, but the way in which ligands change receptor populations to impart signals to cells remains to be determined. In the first of two articles, Terry Kenakin discusses a basic question in receptor pharmacology, namely the nature of ligand efficacy.
关于药物对受体蛋白作用的描述基于用于描述分子与惰性表面质量作用动力学的模型和方程。这些模型对药物亲和力给出了充分的描述,即一个分子与受体蛋白结合的程度,但配体如何改变受体群体以向细胞传递信号仍有待确定。在两篇文章的第一篇中,特里·凯纳金讨论了受体药理学中的一个基本问题,即配体效能的本质。