[18F]GBR 13119在体内与脑多巴胺摄取系统的结合
In vivo binding of [18F]GBR 13119 to the brain dopamine uptake system.
作者信息
Kilbourn M R
机构信息
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.
出版信息
Life Sci. 1988;42(14):1347-53. doi: 10.1016/0024-3205(88)90163-4.
Regional rat brain uptake of [18F]GBR 13119, a high specific activity, positron-emitter labeled derivative of the potent dopamine uptake antagonist GBR 12935, is reported. Striatum to cerebellum ratios of 3 are obtained at 90 minutes post injection. Specific binding in striatum can be blocked by pretreatment with dopamine uptake system antagonists (mazindol, nomifensine) but not with receptor antagonists (spiperone, flupenthixol). [18F]GBR 13119 is proposed as a new positron-emitting radioligand for in vivo PET studies of the pre-synaptic dopamine uptake system.
据报道，强效多巴胺摄取拮抗剂GBR 12935的高比活度、正电子发射体标记衍生物[18F]GBR 13119在大鼠脑内的区域摄取情况。注射后90分钟时，纹状体与小脑的比值为3。纹状体内的特异性结合可被多巴胺摄取系统拮抗剂（吗茚酮、诺米芬辛）预处理阻断，但不能被受体拮抗剂（螺哌隆、氟哌噻吨）阻断。[18F]GBR 13119被提议作为一种新的正电子发射放射性配体，用于突触前多巴胺摄取系统的体内PET研究。
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