Quantitative Analysis for Estimating Binding Potential of the Brain Serotonin Transporter with [11C]McN5652

Quantitative Analysis for Estimating Binding Potential of the Brain Serotonin Transporter with [11C]McN5652
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定量分析估计脑血清素转运蛋白与 [11C]McN5652 的结合潜力

DOI:
10.1097/00004647-200204000-00013
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发表时间:
2002
影响因子:
6.3
通讯作者:
Kazutoshi Suzuki
Kazutoshi Suzuki
中科院分区:
医学1区
文献类型:
--
作者:
Y. Ikoma;T. Suhara;H. Toyama;T. Ichimiya;A. Takano;Y. Sudo;M. Inoue;F. Yasuno;Kazutoshi Suzuki

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[11C](+)McN5652 是一种选择性血清素再摄取抑制剂,对血清素转运蛋白具有亚纳摩尔效力,目前用于正电子发射断层扫描研究。然而,由于其复杂的特性,体内区域[11C](+)McN5652结合潜力的定量是一个有争议的问题。作者检查了非特异性结合的区域差异,并提出了估计 [11C](+)McN5652 结合潜力的简单方法。对于非活性异构体 [11C](−)McN5652 和 [11C](+)McN5652 饱和度研究,通过丘脑与小脑的活性比来评估非特异性结合的区域差异。丘脑的分布体积约为小脑的1.16倍。在有或没有动脉输入功能的情况下,通过非线性最小二乘法和图形方法估计丘脑与小脑的分布体积比。不采血的k2′图解法是实用的,最适用于分布体积比的估计,因为该方法在模拟研究中比非线性最小二乘法更稳定。用[11C](+)McN5652的分布体积比估计的结合潜力和用[11C](−)McN5652的分布体积比校正代表了评估血清素转运蛋白结合的最可靠的参数。
[11C](+)McN5652 is a selective serotonin reuptake inhibitor with subnanomolar potency for the serotonin transporter, and is currently being used for positron emission tomography studies. However, quantification of the regional [11C](+)McN5652 binding potential in vivo is a controversial issue because of its complex characteristics. The authors examined the regional differences in nonspecific binding and proposed simple methods for estimating the binding potential of [11C](+)McN5652. The regional difference in nonspecific binding was evaluated by the activity ratio of the thalamus compared with the cerebellum for inactive-isomer [11C](−)McN5652 and [11C](+)McN5652 saturation studies. The distribution volume of the thalamus was approximately 1.16 times larger than that of the cerebellum. The thalamus-to-cerebellum distribution volume ratio was estimated by nonlinear least square and graphical methods, with and without arterial input function. The graphical method with k2′ without blood sampling was practical and most applicable for estimation of the distribution volume ratio because this method is more stable than the nonlinear least square method in the simulation study. Binding potential estimated with the distribution volume ratio of [11C](+)McN5652 and the correction with distribution volume ratio of [11C](−)McN5652 represent the most reliable parameters for the assessment of serotonin transporter binding.
[11C]( )McN5652 作为放射性示踪剂,用于使用 PET 对血清素摄取部位进行成像。
DOI: 10.1016/0024-3205(93)90440-e
发表时间: 1993
期刊: Life sciences
影响因子: 6.1
作者:
Suehiro,M;Scheffel,U;Ravert,HT;Dannals,RF;WagnerJr,HN
通讯作者: WagnerJr,HN
用于研究血清素摄取位点的 PET 放射性示踪剂:carbon-11-McN-5652Z。
DOI: --
发表时间: 1993
期刊: Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子: --
作者:
Suehiro,M;Scheffel,U;Dannals,RF;Ravert,HT;Ricaurte,GA;WagnerJr,HN
通讯作者: WagnerJr,HN
DOI: 10.1016/s0969-8051(00)00137-2
发表时间: 2000-10-01
影响因子: 3.1
作者:
Logan, J
通讯作者: Logan, J
使用 [11C]McN 5652 对人脑血清素转运蛋白进行体内定量。
DOI: --
发表时间: 2000
期刊: Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子: --
作者:
Parsey,RV;Kegeles,LS;Hwang,DR;Simpson,N;Abi-Dargham,A;Mawlawi,O;Slifstein,M;VanHeertum,RL;Mann,JJ;Laruelle,M
通讯作者: Laruelle,M