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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >[ 125I]SD-7015 reveals fine modalities of CB 1 cannabinoid receptor density in the prefrontal cortex during progression of Alzheimer's disease
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[ 125I]SD-7015 reveals fine modalities of CB 1 cannabinoid receptor density in the prefrontal cortex during progression of Alzheimer's disease

机译：[125I] SD-7015显示了阿尔茨海默氏病进展过程中前额叶皮层中CB 1大麻素受体密度的精细模式

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摘要

The cannabinoid type-1 receptor (CB 1R) is one of the most abundant members of the G protein-coupled receptor family in the central nervous system. Once activated by their cognate ligands, endocannabinoids, CB 1Rs generally limit the timing of neurotransmitter release at many cortical synapses. Prior studies have indicated the involvement of CB 1R in neurodegeneration and in various neuronal insults, with an emphasis on their neuroprotective role. In the present study we used a novel selective CB 1R radioligand to investigate regional variations in CB 1R ligand binding as a factor of progressive Braak tau pathology in the frontal cortex of Alzheimer's disease (AD) patients. The frontal cortex was chosen for this study due to the high density of CB 1Rs and their well-characterized involvement in the progression of AD. Post-mortem prefrontal cortex samples from AD patients from Braak stages I to VI and controls were subjected to CB 1R autoradiography with [ 125I]SD-7015 as radioligand. Regional concentration of [ 125I]SD-7015, corresponding to, and thereby representing, regional CB 1R densities, were expressed in fM/g-tissue. The results show that CB 1R density inversely correlates with Braak tau pathology with the following tendency: controls AD Braak stage V-VI AD Braak stage III-IV AD Braak stage I-II. Differences were significant between control and AD Braak stage I-II groups, as well as between controls and the AD group comprising all Braak stages. These findings indicate an up-regulation of the tissue binding of the selective CB 1R radioligand [ 125I]SD7015 in human brains, allowing the detection of fine modalities of receptor expression and radioligand binding during the progression of AD.
机译：大麻素1型受体（CB 1R）是中枢神经系统中G蛋白偶联受体家族中最丰富的成员之一。一旦被其同源配体（内源性大麻素）激活，CB 1R通常会限制许多皮质突触释放神经递质的时间。先前的研究表明CB 1R参与神经变性和各种神经元损伤，并着重于其神经保护作用。在本研究中，我们使用新型的选择性CB 1R放射性配体来研究CB 1R配体结合的区域变化，这是阿尔茨海默病（AD）患者额叶皮质进行性Braak tau病理的一个因素。由于CB 1Rs的高密度及其在AD进程中的良好特征参与，因此选择了额叶皮层进行本研究。从Braak I至VI阶段的AD患者和对照的死后前额叶皮层样品接受CB 1R放射自显影，其中[125I] SD-7015为放射性配体。以fM / g-组织表示[125 I] SD-7015的区域浓度，对应并因此代表区域CB 1R密度。结果表明，CB 1R密度与Braak tau病理呈负相关，具有以下趋势：对照

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