[11C]β‐CIT‐FE, a radioligand for quantitation of the dopamine transporter in the living brain using positron emission tomography
[11C]β‐CIT‐FE, a radioligand for quantitation of the dopamine transporter in the living brain using positron emission tomography
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[11C]β-CIT-FE，一种放射性配体，用于使用正电子发射断层扫描对活体大脑中的多巴胺转运蛋白进行定量
DOI：
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发表时间：
1996
期刊：
影响因子：
--
通讯作者：
C. Swahn
中科院分区：
文献类型：
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作者：
C. Halldin;L. Farde;C. Lundkvist;N. Ginovart;Y. Nakashima;P. Karlsson;C. Swahn
可卡因类似物β-CIT-FE（N-（2-氟乙基）-2 β-甲氧羰基-3 β-（4-碘苯基）去甲托烷）用11 C标记，用于多巴胺转运蛋白的正电子发射断层扫描（PET）研究。食蟹猴静脉给药后，[11 C]β-CIT-FE在纹状体中蓄积，60 min后纹状体与小脑的比值约为9。在30-50 min内达到纹状体中特异性[11 C]β-CIT-FE结合的假平衡。丘脑与小脑和新皮质与小脑的放射性比值分别约为2和1.5。在置换和预处理实验中，注射β-CIT或多巴胺转运蛋白抑制剂GBR 12909后，纹状体中的放射性降低，但小脑中的放射性未降低，表明注射[11 C]β-CIT-FE后的纹状体放射性代表与多巴胺转运蛋白位点的可逆结合。在用可卡因替代或预处理后，不仅在纹状体，而且在丘脑和新皮质中也有显着的作用。[11C]β-CIT-FE有可能作为一种有用的PET放射性配体，用于定量体内灵长类动物脑中的多巴胺转运蛋白。© 1996 Wiley利斯公司
The cocaine analogue β‐CIT‐FE (N‐(2‐fluoroethyl)‐2β‐carbomethoxy‐3β‐(4‐iodophenyl)nortropane) was labeled with 11C for positron emission tomography (PET) studies of the dopamine transporter. After intravenous administration to a cynomolgus monkey, [11C]β‐CIT‐FE accumulated in the striatum with a striatum‐to‐cerebellum ratio of about 9 after 60 min. Pseudoequilibrium of specific [11C]β‐CIT‐FE binding in the striatum was obtained within 30–50 min. The radioactivity ratios of the thalamus to the cerebellum and the neocortex to the cerebellum were about 2 and 1.5, respectively. In displacement and pretreatment experiments, radioactivity in the striatum but not in the cerebellum was reduced after injection of β‐CIT or the dopamine transporter inhibitor GBR 12909, indicating that striatal radioactivity following injection of [11C]β‐CIT‐FE represents reversible binding to dopamine transporter sites. After displacement or pretreatment with cocaine there was a marked effect not only in the striatum but also in the thalamus and neocortex. [11C]β‐CIT‐FE has potential as a useful PET radioligand for quantitation of the dopamine transporter in the primate brain in vivo. © 1996 Wiley‐Liss, Inc.
[123I]-2 beta-甲甲氧基-3 beta-(4-碘苯基)托烷：大脑中单胺再摄取位点的高亲和力 SPECT 放射性示踪剂。
影响因子：
7.3
作者：
Neumeyer,JL;Wang,SY;Milius,RA;Baldwin,RM;Zea-Ponce,Y;Hoffer,PB;Sybirska,E;al-Tikriti,M;Charney,DS;Malison,RT
通讯作者：
Malison,RT
[11C] beta-CIT，可卡因类似物。
影响因子：
3.1
作者：
Müller,L;Halldin,C;Farde,L;Karlsson,P;Hall,H;Swahn,CG;Neumeyer,J;Gao,Y;Milius,R
通讯作者：
Milius,R