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Pittsburg 化合物 B 在人体中的血脑传递。

Blood-brain transfer of Pittsburgh compound B in humans.

机构信息

Department of Neuroscience and Pharmacology, University of Copenhagen Copenhagen, Denmark ; Department of Nuclear Medicine and PET Centre, Aarhus University Hospital Aarhus, Denmark ; Center of Functionally Integrative Neuroscience, Faculty of Health, Aarhus University Aarhus, Denmark ; Department of Neurology, McGill University Montreal, QC, Canada ; Department of Radiology and Radiological Science, Johns Hopkins University Baltimore, MD, USA.

出版信息

Front Aging Neurosci. 2013 Nov 7;5:70. doi: 10.3389/fnagi.2013.00070. eCollection 2013.

DOI:10.3389/fnagi.2013.00070
PMID:24223554
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3819578/
Abstract

In the labeled form, the Pittsburgh compound B (2-(4'-{N-methyl-[(11)C]}methyl-aminophenyl)-6-hydroxy-benzothiazole, [(11)C]PiB), is used as a biomarker for positron emission tomography (PET) of brain β-amyloid deposition in Alzheimer's disease (AD). The permeability of [(11)C]PiB in the blood-brain barrier is held to be high but the permeability-surface area product and extraction fractions in patients or healthy volunteers are not known. We used PET to determine the clearance associated with the unidrectional blood-brain transfer of [(11)C]PiB and the corresponding cerebral blood flow rates in frontal lobe, whole cerebral cortex, and cerebellum of patients with Alzheimer's disease and healthy volunteers. Regional cerebral blood flow rates differed significantly between the two groups. Thus, regional and whole-brain permeability-surface area products were identical, in agreement with the observation that numerically, but insignificantly, unidirectional blood-brain clearances are lower and extraction fractions higher in the patients. The evidence of unchanged permeability-surface area products in the patients implies that blood flow changes can be deduced from the unidirectional blood-brain clearances of [(11)C]PiB in the patients.

摘要

在标记形式中,匹兹堡化合物 B(2-(4'-{N-甲基-[(11)C]}甲氨基苯基)-6-羟基苯并噻唑,[(11)C]PiB)被用作阿尔茨海默病(AD)脑β-淀粉样蛋白沉积的正电子发射断层扫描(PET)的生物标志物。[(11)C]PiB 在血脑屏障中的通透性被认为是高的,但在患者或健康志愿者中的通透性表面积产物和提取分数尚不清楚。我们使用 PET 来确定与 [(11)C]PiB 的单向血脑转移相关的清除率,以及额叶、整个大脑皮层和小脑的相应脑血流率。两组之间的区域脑血流率存在显著差异。因此,区域性和全脑通透性表面积产物是相同的,这与观察结果一致,即数值上但无统计学意义,患者的单向血脑清除率较低,提取分数较高。患者中通透性表面积产物不变的证据表明,血流变化可以从患者的 [(11)C]PiB 的单向血脑清除率中推断出来。

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