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使用相同化合物作为放射性配体和竞争剂,通过结合实验计算受体数量。

Calculating receptor number from binding experiments using same compound as radioligand and competitor.

作者信息

DeBlasi A, O'Reilly K, Motulsky H J

出版信息

Trends Pharmacol Sci. 1989 Jun;10(6):227-9. doi: 10.1016/0165-6147(89)90266-6.

Abstract

Saturation experiments using increasing concentrations of radioligand are commonly used to determine receptor number and affinity, but this protocol is not feasible in all situations. Alternatively, competitive binding experiments are often performed in which binding of a single concentration of radioligand is completed for by multiple concentrations of the same unlabelled ligand, but the analysis of such data has been difficult. Antonio DeBlasi and colleagues present here a simple method for calculating receptor number and affinity from competitive binding data. This experimental protocol is useful when a single class of binding site is present, but is often not able to detect the presence of two classes of site.

摘要

使用浓度递增的放射性配体进行饱和实验通常用于确定受体数量和亲和力,但该方案并非在所有情况下都可行。另外,常进行竞争性结合实验,即单一浓度的放射性配体与多种浓度的相同未标记配体竞争结合,但此类数据分析一直很困难。安东尼奥·德布拉西及其同事在此提出了一种从竞争性结合数据计算受体数量和亲和力的简单方法。当存在单一类别的结合位点时,该实验方案很有用,但通常无法检测到两类位点的存在。

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