Synthesis of (S)-N-[methyl-11C]nicotine and its regional distribution in the mouse brain: a potential tracer for visualization of brain nicotinic receptors by positron emission tomography.
Synthesis of (S)-N-[methyl-11C]nicotine and its regional distribution in the mouse brain: a potential tracer for visualization of brain nicotinic receptors by positron emission tomography.
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(S)-N-[甲基-11C]尼古丁的合成及其在小鼠大脑中的区域分布：通过正电子发射断层扫描可视化大脑烟碱受体的潜在示踪剂。
DOI：
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发表时间：
1992
影响因子：
1.7
通讯作者：
A. Yokoyama
中科院分区：
文献类型：
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作者：
H. Saji;Y. Magata;Y. Yamada;K. Tajima;Y. Yonekura;J. Konishi;Y. Ohmomo;A. Yokoyama
用[11 C]-碘甲烷在二甲基甲酰胺-二甲基亚砜中对（S）-去甲烟碱进行N-甲基化反应，合成了烟碱激动剂11 C-标记（S）-烟碱，用于正电子发射断层扫描（PET）研究人脑烟碱受体。该N-甲基化反应的放化产率在5 min内大于90%，产物经高效液相色谱纯化后，放化纯度大于99%，比放射性为7.4- 11.1GBq/μ mol。比较了静脉注射（S）-[11 C]尼古丁与（R）-[11 C]尼古丁在小鼠脑中的区域分布。注射（S）-[11 C]尼古丁后，放射性摄取的区域顺序为：皮质>丘脑>海马>纹状体>下丘脑>小脑。此外，（S）-[11 C]尼古丁被未标记的（S）-尼古丁从大脑中取代，但未标记的（R）-尼古丁未引起摄取变化。相比之下，（R）-[11 C]尼古丁显示出较低的脑摄取和较小的放射性区域差异。
A nicotine agonist, 11C-labeled (S)-nicotine, was synthesized by N-methylation of (S)-nornicotine with [11C]-methyl iodide in dimethylformamide-dimethylsulfoxide in order to study nicotinic receptors in the human brain by positron emission tomography. The radiochemical yield of this N-methylation reaction was more than 90% within 5 min. After purification by high performance liquid chromatography the radiochemical purity of the product was more than 99% and the specific radioactivity was 7.4-11.1 GBq/mumol. The regional distribution of (S)-[11C]nicotine in the mouse brain after intravenous injection was compared with that of (R)-[11C]nicotine. After injection of (S)-[11C]nicotine, the regional uptake of radioactivity was in the following order: cortex greater than thalamu approximately hippocampus greater than striatum greater than hypothalamus greater than cerebellum. Moreover, (S)-[11C]nicotine was displaced from the brain by unlabeled (S)-nicotine, but unlabeled (R)-nicotine caused no change in uptake. In contrast, (R)-[11C]nicotine showed a lower brain uptake and lesser regional differences in radioactivity.