Van der Graaf P H
Leiden/Amsterdam Center for Drug Research , Division of Pharmacology, Leiden, The Netherlands.
J Pharmacol Toxicol Methods. 1998 Nov;40(4):241-3. doi: 10.1016/s1056-8719(99)00011-8.
Recently, Calderone and Martinotti (J Pharmacol Toxicol Meth 40:57-62, 1998) presented a simple equation for the estimation of agonist dissociation equilibrium constants from data obtained from receptor inactivation experiments using an irreversible, competitive antagonist. In the present paper, however, it is demonstrated that application of this equation will result in significant over- and underestimation of agonist affinity in the case of flat and steep concentration-effect curves, respectively. Therefore, accurate estimation of agonist affinity using irreversible receptor inactivation requires detailed curve-shape information from both control and antagonist-treated tissues.
最近，卡尔德龙和马蒂诺蒂（《药理学与毒理学方法杂志》40:57 - 62，1998年）提出了一个简单的方程，用于根据使用不可逆竞争性拮抗剂的受体失活实验所获得的数据来估算激动剂解离平衡常数。然而，在本文中表明，在浓度 - 效应曲线平缓及陡峭的情况下，应用该方程分别会导致对激动剂亲和力的显著高估和低估。因此，使用不可逆受体失活准确估算激动剂亲和力需要来自对照组织和拮抗剂处理组织的详细曲线形状信息。
