[F-18] N-METHYLSPIROPERIDOL - THE RADIOLIGAND OF CHOICE FOR PETT STUDIES OF THE DOPAMINE RECEPTOR IN HUMAN-BRAIN
[F-18] N-METHYLSPIROPERIDOL - THE RADIOLIGAND OF CHOICE FOR PETT STUDIES OF THE DOPAMINE RECEPTOR IN HUMAN-BRAIN
复制标题
DOI：
10.1016/0024-3205(85)90041-4
复制
发表时间：
1985-01-01
期刊：
影响因子：
6.1
通讯作者：
MCPHERSON, DW
中科院分区：
文献类型：
--
作者：
ARNETT, CD;FOWLER, JS;MCPHERSON, DW
N-甲基螺哌利多，酰胺N-甲基类似物的神经安定剂螺哌利多，放射性标记的氟-18，其分布在狒狒的大脑进行了研究，使用正电子发射轴向断层扫描。通过（-）-或（+）-布他拉莫预处理，在纹状体（但不在小脑）中证明了立体特异性结合。动力学分布与[18F]螺哌利多相似，但绝对纹状体摄取（占给药剂量的百分比）至少高出2倍。注射后10 min对狒狒血液的分析表明，血浆中不到一半的放射性是由未改变的放射性配体引起的。对[18 F]-N-甲基螺哌利多在大鼠脑中4 h的代谢稳定性的分析表明，与[18 F]螺哌利多一样，它对大鼠CNS中的代谢转化非常稳定。[18 F]-N-甲基螺哌利多在大鼠纹状体的摄取和保留是[18 F]螺哌利多的5倍。显然，[18F]-N-甲基螺哌啶是研究人类多巴胺受体的理想选择。
N-Methylspiroperidol, the amide N-methyl analog of the neuroleptic spiroperidol, was radiolabeled with fluorine-18, and its distribution in the baboon brain was studied using positron emission transaxial tomography. Stereospecific binding was demonstrated in the striatum (but not in the cerebellum) by pretreatment with (-)- or (+)-butaclamol. The kinetic distribution was similar to that of [18F]spiroperidol, but the absolute striatal uptake (in percent of administered dose) was at least 2-fold higher. Analysis of baboon blood at 10 min after injection indicated that less than half of the radioactivity in the plasma was due to unchanged radioligand. Analysis of the metabolic stability of [18F]-N-methylspiroperidol in rat brain for 4 h indicated that, like [18F]spiroperidol, it is very stable to metabolic transformation in the rat CNS. Striatal uptake and retention in the rat was 5-fold higher for [18F]-N-methylspiroperidol than for [18F]spiroperidol. Apparently, [18F]-N-methylspiroperidol is an ideal choice for studies of the dopamine receptor in humans.