In vivo receptor assay with multiple ligand concentrations:: An equilibrium approach
In vivo receptor assay with multiple ligand concentrations:: An equilibrium approach
复制标题
DOI：
10.1097/00004647-200209000-00011
复制
发表时间：
2002-09-01
影响因子：
6.3
通讯作者：
Doudet, DJ
中科院分区：
文献类型：
--
作者：
Holden, JE;Jivan, S;Doudet, DJ
通过体内PET研究在高配体特异性放射性下测定的配体-受体结合潜力反映了受体密度和配体-受体亲和力。这种模糊性已经解决了各种方法的基础上管理的多个未标记的配体浓度。作者旨在实施和完善一种多配体浓度受体测定方法，该方法结合了最大的简单性和最小的假设和模型依赖性，但仍能可靠地区分密度和亲和力效应。该方法使用大疱给药，然后输注，以获得结合的配体和配体浓度的其他组分之间的真正平衡，并且不需要测量血浆中的配体，在正常对照和MPTP中进行的raelo-pride研究的分析中，实施了四种从测量的平衡数据优化所需密度和亲和力参数的方法，并进行了比较。有病变的非人类灵长类动物作者得出结论，该方法对于常规使用来说足够简单，但对于正在进行的多巴胺系统慢性和急性药物作用的研究来说足够可靠。
The ligand-receptor binding potential determined by in vivo PET studies at high ligand-specific radioactivity reflects both the receptor density and ligand-receptor affinity. This ambiguity has been resolved by various methods based on the administration of multiple unlabeled ligand concentrations. The authors aimed to implement and refine an approach to multiple ligand concentration receptor assay that combined maximum simplicity and a minimum of assumptions and model dependence that would nonetheless reliably distinguish density from affinity effects. The approach uses administration by bulus followed by infusion to obtain a true equilibrium between bound ligand and the other components of the ligand concentration, and does not require measurements of ligand in blood plasma, Four approaches to the optimization of the desired density and affinity parameters from the measured equilibrium data were implemented and compared in the analysis of raelo-pride studies performed in both normal control and MPTP-lesioned nonhuman primates. The authors conclude that the method is simple enough for routine use and yet reliable enough to apply in ongoing studies of both chronic and acute drug effects in the dopamine system.