Kuikka J T, Baulieu J L, Hiltunen J, Halldin C, Bergström K A, Farde L, Emond P, Chalon S, Yu M, Nikula T, Laitinen T, Karhu J, Tupala E, Hallikainen T, Kolehmainen V, Mauclaire L, Maziere B, Tiihonen J, Guilloteau D
Department of Clinical Physiology, Kuopio University Hospital, FIN-70210 Kuopio, Finland.
Eur J Nucl Med. 1998 May;25(5):531-4. doi: 10.1007/s002590050254.
The iodine-123 labelled selective ligand N-(3-iodoprop-2E-enyl)-2-beta-carbomethoxy-3beta-(4-methylphenyl) nortropane ([123I]PE2I) was evaluated as a probe for in vivo dopamine transporter imaging in the human brain. Six healthy subjects were imaged with a high-resolution single-photon emission tomography scanner. Striatal radioactivity peaked at 1 h after injection. The background radioactivity was low. The volume of distribution in the striatum was 94+/-24 ml/ml. The results were compared with those of [123I]beta-CIT imaging. There was no significant uptake of [123I]PE2I in serotonin-rich regions such as the midbrain, hypothalamus and anterior gingulus, suggesting that in vivo binding is specific for the dopamine transporter. One main polar metabolite of [123I]PE2I was found in plasma, and the parent plasma concentration decayed rapidly. Radiation exposure to the study subject is 0.022+/-0.004 mSv/MBq (effective dose). The preliminary results suggest that [123I]PE2I is a selective SPET ligand for imaging striatal dopamine transporter density.
对碘-123标记的选择性配体N-(3-碘代丙-2E-烯基)-2-β-甲氧基羰基-3β-(4-甲基苯基)降托烷([123I]PE2I)进行了评估，作为人脑活体多巴胺转运体成像的一种探针。6名健康受试者用高分辨率单光子发射断层扫描仪进行成像。纹状体放射性在注射后1小时达到峰值。本底放射性较低。纹状体中的分布容积为94±24 ml/ml。将结果与[123I]β-CIT成像结果进行比较。在富含5-羟色胺的区域如中脑、下丘脑和前扣带回中，[123I]PE2I没有明显摄取，提示活体结合对多巴胺转运体具有特异性。在血浆中发现了[123I]PE2I的一种主要极性代谢物，母体血浆浓度迅速衰减。研究对象所受辐射剂量为0.022±0.004 mSv/MBq(有效剂量)。初步结果表明，[123I]PE2I是一种用于纹状体多巴胺转运体密度成像的选择性单光子发射断层配体。
