Blin J, Pappata S, Kiyosawa M, Crouzel C, Baron J C
Service Hospitalier Frédéric Joliot, CEA, Département de Biologie, Orsay, France.
Eur J Pharmacol. 1988 Feb 16;147(1):73-82. doi: 10.1016/0014-2999(88)90635-8.
The potential usefulness of 18F-labelled setoperone, a high-affinity antagonist of the serotonin-2 (S2) receptors, to study the S2 receptors in vivo with positron emission tomography (PET) was investigated in four baboons. In the control state, there was a rapid wash-out of intravenously injected tracer from the cerebellum, a structure essentially devoid of S2, receptors, and marked retention in both the cerebral cortex and the striatum (region/cerebellum ratios up to 3 and 3.5 after 60 min in cortex and striatum, respectively). The retention of radioligand in the cerebral cortex was abolished after pretreatment with spiperone or ketanserin at saturating doses. In striatum, however, radioligand retention was fully prevented by spiperone but only partly by ketanserin. These results demonstrate that [18F]setoperone was bound to the S2 receptors in the cerebral cortex, whereas the radioligand was bound to both the S2 and the dopamine D2 receptors in the striatum. The high cortex/cerebellum ratio achieved indicates that [18F]setoperone should be a useful radiotracer for PET studies of the S2 receptors.
在四只狒狒身上研究了18F标记的舍托哌隆（一种5-羟色胺-2（S2）受体的高亲和力拮抗剂）利用正电子发射断层扫描（PET）在体内研究S2受体的潜在效用。在对照状态下，静脉注射的示踪剂能迅速从小脑（一个基本没有S2受体的结构）中清除，而在大脑皮层和纹状体中则有明显滞留（在皮层和纹状体中60分钟后区域/小脑比值分别高达3和3.5）。用饱和剂量的螺哌隆或酮色林预处理后，放射性配体在大脑皮层的滞留被消除。然而，在纹状体中，螺哌隆能完全阻止放射性配体的滞留，而酮色林只能部分阻止。这些结果表明，[18F]舍托哌隆与大脑皮层中的S2受体结合，而放射性配体与纹状体中的S2和多巴胺D2受体都结合。所达到的高皮层/小脑比值表明，[18F]舍托哌隆应该是用于S2受体PET研究的一种有用的放射性示踪剂。
