Clarke W P, Bond R A
Department of Pharmacology, University of Texas Health Science Center at San Antonio 78284-7764, USA.
Trends Pharmacol Sci. 1998 Jul;19(7):270-6. doi: 10.1016/s0165-6147(97)01138-3.
In the discipline of pharmacology, drugs (ligands) are used as tools to elucidate the processes of biological systems. Because of this, pharmacologists strive to delineate all characteristics of drugs. Decades of research have resulted in the proposal that ligands possess two properties that are intrinsic to the ligand and are invariant of the system in which their effects are investigated. These properties are affinity (the capacity of a drug to bind to a receptor) and intrinsic efficacy (the capacity of a drug to activate or inactivate a receptor). Although affinity is a relatively easy parameter to measure with a variety of techniques, ways of quantifying intrinsic efficacy have remained elusive ever since its inception. Furthermore, recent evidence suggests that intrinsic efficacy might not be a single, ligand-dependent parameter but that agonists might have multiple intrinsic efficacies. William Clarke and Richard Bond discuss several reasons why the claim that intrinsic efficacy is a ligand-dependent parameter should be questioned, and the possible impact of these findings.
在药理学领域，药物（配体）被用作阐明生物系统过程的工具。因此，药理学家努力描绘药物的所有特性。数十年的研究提出，配体具有两种内在特性，且与其作用所研究的系统无关。这些特性是亲和力（药物与受体结合的能力）和内在活性（药物激活或失活受体的能力）。虽然亲和力是一个相对容易用多种技术测量的参数，但自内在活性概念提出以来，量化它的方法一直难以捉摸。此外，最近的证据表明，内在活性可能不是一个单一的、依赖于配体的参数，而是激动剂可能具有多种内在活性。威廉·克拉克和理查德·邦德讨论了几个理由，说明为何内在活性是依赖于配体的参数这一说法应受到质疑，以及这些发现可能产生的影响。
