Parameter and index images of benzodiazepine receptor concentration in the brain.

Parameter and index images of benzodiazepine receptor concentration in the brain.
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大脑中苯二氮卓受体浓度的参数和指数图像。

DOI:
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发表时间:
1995
影响因子:
9.3
通讯作者:
A. Syrota
A. Syrota
中科院分区:
医学1区
文献类型:
--
作者:
P. Millet;J. Delforge;F. Mauguière;S. Pappatà;L. Cinotti;V. Frouin;Y. Samson;B. Bendriem;A. Syrota

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未标记 体内研究的配体-受体相互作用与PET数据是基于不同的方法,提供定量结果(受体密度和亲和力)或指数,被认为是与受体浓度。本研究的目的是获得苯二氮卓受体浓度和氟马西尼亲和力的参数图像,并研究两个受体浓度指标的有效性。 方法 一个三室配体-受体模型,[11 C]氟马西尼,并使用三注射协议在人类志愿者中获得的实验数据被用来获取参数图像。还测试了延迟活性法和表观分布体积(使用二室模型估计),并将其结果与多次注射法的结果进行了比较。 结果 获得了受体密度、亲和力和所有动力学参数的参数图像,变异系数可接受。发现受体密度与表观亲和力之间存在相关性(r = 0.83; p < 0.0005)。受体浓度和表观分布体积之间的相关性(分别用三房室模型和二房室模型估计)使用线性(通常假设)和非线性相关性(源自受体密度和亲和力之间的关系)进行评估。 结论 尽管这个协议的复杂性(三次注射,2小时的实验,血液采样和代谢物研究),我们表明,多次注射的方法是适合参数脑成像。通过使用这种方法作为参考,我们推断,分布体积和延迟活动图像是有效的方法,在通常范围内的苯二氮卓类受体的浓度在人脑中发现。
UNLABELLED In vivo studies of ligand-receptor interactions with PET data are based on different approaches that provide either quantitative results (receptor density and affinity) or indices that are assumed to be correlated with the receptor concentration. The aims of this study are to obtain parametric images of benzodiazepine receptor concentration and of flumazenil affinity and to study the validity of two receptor concentration indexes. METHODS A three-compartment ligand-receptor model, [11C]flumazenil, and experimental data obtained using a three-injection protocol in human volunteers were used to acquire parametric images. The delayed activity method and the apparent distribution volume (estimated using a two-compartment model) were also tested and their results compared with those of the multi-injection approach. RESULTS Parametric images of receptor density, affinity and all kinetic parameters were obtained with acceptable variation coefficients. A correlation between receptor density and apparent affinity was found (r = 0.83; p < 0.0005). The correlation between receptor concentration and apparent distribution volume (estimated with three- and two-compartment models, respectively) was accessed using both a linear (the usual hypothesis) and a nonlinear correlation derived from the relationship between the receptor density and the affinity. CONCLUSION In spite of the complexity of this protocol (three injections, a 2-hr experiment, blood sampling and a metabolite study), we showed that the multi-injection approach is suitable for parametric brain imaging. By using this approach as a reference, we deduced that the distribution volume and delayed activity images are valid methods in the usual range of the benzodiazepine receptor concentrations found in the human brain.