Titus E O
Naunyn Schmiedebergs Arch Pharmacol. 1975;288(2-3):269-81. doi: 10.1007/BF00500532.
The isolation of macromolecules that bind drugs and neurohumoral mediators at receptor sites will require analytical methods adequate to detect these substances in homogenates and crude mixtures. Although the binding of isotopically labeled agonists has been useful in a few instances, equilibrium binding studies of radioactive, lipophilic antagonists promises to be more useful with beta-adrenergic receptors. Alkylation by radioactive reagents that seek out specific receptors or specific functional groups on protein have been used in attempts to label other receptors. Conformationally directed labeling of receptor and receptor-related proteins by the latter group of alkylating agents has been used with receptors for cardiac glycosides and may be applicable to other systems.
在受体位点分离与药物和神经体液介质结合的大分子，将需要足以在匀浆和粗混合物中检测这些物质的分析方法。尽管同位素标记激动剂的结合在少数情况下有用，但放射性亲脂性拮抗剂的平衡结合研究有望在β-肾上腺素能受体研究中更有用。利用寻找蛋白质上特定受体或特定官能团的放射性试剂进行烷基化，已被用于尝试标记其他受体。后一类烷基化剂对受体及受体相关蛋白进行构象导向标记已用于强心苷受体，也可能适用于其他系统。
