In Vivo and In Vitro Imaging of I2 Imidazoline Receptors in the Monkey Brain

In Vivo and In Vitro Imaging of I2 Imidazoline Receptors in the Monkey Brain
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DOI:
10.1002/syn.20897
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发表时间:
2011-05-01
期刊:
影响因子:
2.3
通讯作者:
Zhang, Ming-Rong
Zhang, Ming-Rong
中科院分区:
医学4区
文献类型:
--
作者:
Kawamura, Kazunori;Maeda, Jun;Zhang, Ming-Rong

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I-2咪唑啉受体(I(2)Rs)与抑郁症、阿尔茨海默病和亨廷顿病有关。然而,到目前为止,I(2)Rs在猴子大脑中的活体成像还没有报道。我们用C-11标记的2-(3-氟-4-甲苯基)-4,5-二氢-1H-咪唑([C-11]FTIMD)在猴脑中进行了(I(2)Rs)的体外和体内成像,[C-11]FTIMD对I(2)Rs具有高选择性亲和力。在一项自动放射成像(ARG)研究中,[C-11]FTIMD在猴脑中的分布模式类似于[H-3]咪唑克生在人脑中结合I(2)Rs的分布模式,如前所述。[C-11]FTIMD的特异性结合占存在I(2)Rs的脑区总结合的97%。在正电子发射断层扫描(PET)研究中,放射性在存在I(2)Rs配体BU224的脑区积聚,在注射[C-11]FTIMD后15-45分钟,累积的放射性降至基线的66%-75%。这些结果表明,[C-11]FTIMD在猴脑中显示了与I(2)Rs的特异性结合,如PET和ARG所描绘的那样。我们使用[C-11]FTIMD在猴子大脑中进行了第一次体内I(2)Rs成像。Synapse 65:452-455,2011。(C)2010年Wiley-Liss公司
I-2 imidazoline receptors (I(2)Rs) are associated with depression, Alzheimer's disease, and Huntington's disease. However, in vivo imaging of I(2)Rs in the monkey brain has not been reported until now. We performed in vitro and in vivo imaging of (I(2)Rs) in the monkey brain using C-11-labeled 2-(3-fluoro-4-tolyl)-4,5-dihydro-1H-imidazole ([C-11]FTIMD) which has high and selective affinity of I(2)Rs. In an auto-radiography (ARG) study, the distribution pattern of [C-11]FTIMD in the monkey brain was similar to that of [H-3] idazoxan binging to I(2)Rs in the human brain, which was previously described. The specific binding of [C-11]FTIMD accounted for > 97% of total binding in brain regions existing I(2)Rs. In positron emission tomography (PET) studies, the radioactivity was accumulated in brain regions existing I(2)Rs ligand BU224, the accumulated radioactivity was decreased to approximately 66%-75% of the baseline measurement at 15-45 min after injection of [C-11]FTIMD. These results suggest that [C-11]FTIMD shows the specific-binging to I(2)Rs in the monkey brain as depicted by PET and ARG. We performed the first in vivo imaging of I(2)Rs using [C-11]FTIMD in the monkey brain. Synapse 65: 452-455, 2011. (C)2010 Wiley-Liss, Inc.