[123I]表哌立登的代谢可能会影响单光子发射断层扫描对脑多巴胺D2受体的成像。

Metabolism of [123I]epidepride may affect brain dopamine D2 receptor imaging with single-photon emission tomography.

作者信息

Bergström K A, Yu M, Kuikka J T, Akerman K K, Hiltunen J, Lehtonen J, Halldin C, Tiihonen J

机构信息

Department of Clinical Physiology and Nuclear Medicine, Kuopio University Hospital, Finland.

出版信息

Eur J Nucl Med. 2000 Feb;27(2):206-8. doi: 10.1007/s002590050028.

DOI:10.1007/s002590050028

PMID:10755727

Abstract

Iodine-123 labelled epidepride is a novel radiopharmaceutical for the study of cerebral dopamine D2 receptors using single-photon emission tomography (SPET). A lipophilic labelled metabolite of [123I]epidepride which may enter the brain and hamper the quantitation of receptors has been observed in human plasma. In the present study, gradient high-performance liquid chromatography (HPLC) was used to investigate the plasma concentration of the lipophilic labelled metabolite and its correlation to SPET imaging of striatal dopamine D2 receptors. A linear regression fit showed a negative correlation between the amount of the lipophilic labelled metabolite and the striatum to cerebellum ratio (n=16, R=-0.58, P<0.02), suggesting that plasma metabolite analysis is essential when imaging dopamine D2 receptors with SPET using [123I]epidepride.

摘要

碘 - 123标记的表哌立得是一种新型放射性药物，用于通过单光子发射断层扫描（SPET）研究脑多巴胺D2受体。在人体血浆中已观察到[123I]表哌立得的一种亲脂性标记代谢物，它可能进入大脑并妨碍受体的定量分析。在本研究中，采用梯度高效液相色谱（HPLC）来研究亲脂性标记代谢物的血浆浓度及其与纹状体多巴胺D2受体SPET成像的相关性。线性回归拟合显示亲脂性标记代谢物的量与纹状体与小脑的比值之间呈负相关（n = 16，R = -0.58，P < 0.02），这表明当使用[123I]表哌立得通过SPET对多巴胺D2受体进行成像时，血浆代谢物分析至关重要。