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使用[羰基-C]佐米曲普坦对恒河猴大脑中5-HT(1B/1D)结合位点进行放射自显影定位。

Autoradiographic Mapping of 5-HT(1B/1D) Binding Sites in the Rhesus Monkey Brain Using [carbonyl-C]zolmitriptan.

作者信息

Lindhe Orjan, Almqvist Per, Kågedal Matts, Gustafsson Sven-Åke, Bergström Mats, Nilsson Dag, Antoni Gunnar

机构信息

Uppsala Imanet AB, GE Healthcare, P.O. Box 967, 751 09 Uppsala, Sweden.

出版信息

Int J Mol Imaging. 2011;2011:694179. doi: 10.1155/2011/694179. Epub 2011 Oct 12.

DOI:10.1155/2011/694179
PMID:22013519
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3195497/
Abstract

Zolmitriptan is a serotonin 5-HT(1B/1D) receptor agonist that is an effective and well-tolerated drug for migraine treatment. In a human positron emission tomography study, [(11)C]zolmitriptan crossed the blood-brain barrier but no clear pattern of regional uptake was discernable. The objective of this study was to map the binding of [(11)C]zolmitriptan in Rhesus monkey brain using whole hemisphere in vitro autoradiography with [(11)C]zolmitriptan as a radioligand. In saturation studies, [(11)C]zolmitriptan showed specific (90%) binding to a population of high-affinity binding sites (Kd 0.95-5.06 nM). There was regional distribution of binding sites with the highest density in the ventral pallidum, followed by the external globus pallidus, substantia nigra, visual cortex, and nucleus accumbens. In competitive binding studies with 5-HT(1) receptor antagonists, [(11)C]zolmitriptan binding was blocked by selective 5-HT(1B) and 5-HT(1D) ligands in all target areas. There was no appreciable change in binding with the addition of a 5-HT(1A) receptor antagonist.

摘要

佐米曲坦是一种血清素5-HT(1B/1D)受体激动剂，是一种治疗偏头痛有效且耐受性良好的药物。在一项人体正电子发射断层扫描研究中，[(11)C]佐米曲坦穿过了血脑屏障，但未发现明显的区域摄取模式。本研究的目的是使用[(11)C]佐米曲坦作为放射性配体，通过全脑半球体外放射自显影技术绘制[(11)C]佐米曲坦在恒河猴脑中的结合图谱。在饱和研究中，[(11)C]佐米曲坦显示出与一群高亲和力结合位点（Kd 0.95 - 5.06 nM）有特异性（90%）结合。结合位点存在区域分布，腹侧苍白球密度最高，其次是外侧苍白球、黑质、视觉皮层和伏隔核。在与5-HT(1)受体拮抗剂的竞争性结合研究中，[(11)C]佐米曲坦的结合在所有靶区域均被选择性5-HT(1B)和5-HT(1D)配体阻断。添加5-HT(1A)受体拮抗剂后，结合没有明显变化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/b0fe8554b6f9/IJMI2011-694179.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/9ca11c2d9652/IJMI2011-694179.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/1e4b8bbee3b2/IJMI2011-694179.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/b0fe8554b6f9/IJMI2011-694179.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/9ca11c2d9652/IJMI2011-694179.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/1e4b8bbee3b2/IJMI2011-694179.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6308/3195497/b0fe8554b6f9/IJMI2011-694179.003.jpg

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