Moerlein S M, Perlmutter J S
Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110.
Neurosci Lett. 1992 Dec 14;148(1-2):97-100. doi: 10.1016/0304-3940(92)90813-m.
3N-(2'-[18F]Fluoroethyl)benperidol ([18F]FEB) an 18F-labeled analogue of the D2 antagonist benperidol, was evaluated as a tracer for positron emission tomography (PET). PET imaging of a living baboon showed that the fluorinated ligand rapidly localized in vivo within D2 receptor-rich brain tissue, with selective retention lasting over 2 h after tracer injection. Pretreatment of the animal with unlabeled D2-specific antagonist eticlopride (4 mg/kg, i.v.) 1 h before [18F]FEB completely abolished the selective disposition of the radioligand, whereas the regional cerebral blood flow, blood volume and peripheral metabolism/protein binding of [18F]FEB were not changed. Tracer localization when the baboon was pretreated with unlabeled ketanserin (0.55 mg/kg, i.v.) or SCH 23390 (1.1 mg/kg, i.v.) was identical to that for the control case, indicating that the [18F]FEB did not bind to S2 of D1 receptors in vivo. [18F]FEB has advantages compared to previously used PET tracers, and may be an excellent radioligand for non-invasive study of D2 receptor binding.
3N-(2'-[18F]氟乙基)苯哌利多([18F]FEB)是D2拮抗剂苯哌利多的一种18F标记类似物，被评估用作正电子发射断层扫描(PET)的示踪剂。对一只活体狒狒进行的PET成像显示，这种氟化配体在体内迅速定位于富含D2受体的脑组织中，在注射示踪剂后，选择性滞留持续超过2小时。在注射[18F]FEB前1小时，用未标记的D2特异性拮抗剂依托必利(4毫克/千克，静脉注射)对动物进行预处理，完全消除了放射性配体的选择性分布，而[18F]FEB的局部脑血流量、血容量以及外周代谢/蛋白质结合未发生变化。当用未标记的酮色林(0.55毫克/千克，静脉注射)或SCH 23390(1.1毫克/千克，静脉注射)对狒狒进行预处理时，示踪剂的定位与对照情况相同，表明[18F]FEB在体内不与D1受体的S2结合。与先前使用的PET示踪剂相比，[18F]FEB具有优势，可能是用于D2受体结合无创研究的一种优秀放射性配体。
