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首页> 外文期刊>International journal of molecular imaging >Autoradiographic Mapping of5-HT1B/1DBinding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan
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Autoradiographic Mapping of5-HT1B/1DBinding Sites in the Rhesus Monkey Brain Using [carbonyl-11C]zolmitriptan

机译：使用[羰基-11C]佐米曲普坦对恒河猴脑中5-HT1B / 1D结合位点的放射自显影图

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摘要

Zolmitriptan is a serotonin5-HT1B/1Dreceptor agonist that is an effective and well-tolerated drug for migraine treatment. In a human positron emission tomography study, [11C]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 [11C]zolmitriptan in Rhesus monkey brain using whole hemispherein vitroautoradiography with [11C]zolmitriptan as a radioligand. In saturation studies, [11C]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-HT1receptor antagonists, [11C]zolmitriptan binding was blocked by selective 5-HT1Band 5-HT1Dligands in all target areas. There was no appreciable change in binding with the addition of a 5-HT1Areceptor antagonist.
机译：佐米曲普坦是5-羟色胺5-HT1B / 1D受体激动剂，是治疗偏头痛的有效且耐受性良好的药物。在一项人类正电子发射断层扫描研究中，[11C]佐米曲普坦穿越了血脑屏障，但没有清晰的区域摄取模式。这项研究的目的是使用[11C]佐米曲普坦作为放射配体，使用全半球体外放射自显影技术绘制恒河猴大脑中[11C]佐米曲普坦的结合图。在饱和度研究中，[11C]佐米曲普坦显示出与高亲和力结合位点（Kd 0.95–5.06MnM）的特异性结合（90％）。腹侧苍白球中结合位点的密度最高，然后是苍白球，黑质，视觉皮层和伏隔核。在与5-HT1受体拮抗剂的竞争性结合研究中，[11C]佐米曲普坦的结合被所有目标区域中的选择性5-HT1Band 5-HT1D配体阻断。加入5-HT1A受体拮抗剂后结合没有明显变化。

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