[11C](+)McN5652 as a radiotracer for imaging serotonin uptake sites with PET.
[11C](+)McN5652 as a radiotracer for imaging serotonin uptake sites with PET.
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[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
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发表时间：
1993
期刊：
影响因子：
6.1
通讯作者：
WagnerJr,HN
中科院分区：
文献类型：
--
作者：
Suehiro,M;Scheffel,U;Ravert,HT;Dannals,RF;WagnerJr,HN
[11C]McN5652是一种高效的5-羟色胺（5-羟色胺）摄取阻断剂，其立体异构体的体内行为被确定，以评估其作为正电子发射断层扫描（PET）成像5-羟色胺摄取部位的放射性示踪剂的效用。经小鼠静脉注射后，与[11C]标记的外消旋混合物相比，[11C](+)McN5652在5-HT摄取位点高密度区域的摄取明显更高，滞留时间更长，而[11C](−)McN5652则迅速被清除。对于[11C](+)-对映体，90分钟时下丘脑与小脑的比值达到6。预注射5mg /kg选择性5- ht摄取阻滞剂帕罗西汀（paroxetine）可抑制[11C](+)McN5652在除小脑外的所有区域的结合，抑制率为45-73%。[11C](−)McN5652在任何区域均未显示特异性结合。[11C]标记的顺式异构体McN5655显示出令人惊讶的低脑穿透性，并且在感兴趣的区域没有明显高于小脑的摄取。这些结果表明[11C](+)McN5652是研究体内5-羟色胺摄取位点的PET放射性示踪剂的有希望的候选者。
Thein vivobehavior of the stereoisomers of [11C]McN5652, a highly potent serotonin (5-HT) uptake blocker, was determined to evaluate their utility as radiotracers for imaging 5-HT uptake sites by positron emission tomography (PET). After intravenous injection into mice, [11C](+)McN5652 showed markedly higher uptake and longer retention in regions with high density of 5-HT uptake sites than the [11C]-labeled racemic mixture, while [11C](−)McN5652 washed out rapidly. With the [11C](+)-enantiomer, the ratio between hypothalamus and cerebellum reached 6 at 90 minutes. The binding of [11C](+)McN5652 was inhibited by 45–73% by pre-injection of 5 mg/kg of paroxetine, a selective 5-HT uptake blocker, in all regions examined except cerebellum where no significant effect of the drug was observed. [11C](−)McN5652 showed no specific binding in any of the regions. The [11C]-labeled cis isomer, [11C]McN5655, revealed surprisingly low brain penetration and showed no significantly higher uptake in regions of interest than cerebellum. These results suggest that [11C](+)McN5652 is a promising candidate as a PET radiotracer for studying 5-HT uptake sitesin vivo.