通过对大鼠的生物分布研究评估，碘-123标记的去甲-β-CIT在体内与5-羟色胺转运体结合。

Iodine-123 labelled nor-beta-CIT binds to the serotonin transporter in vivo as assessed by biodistribution studies in rats.

作者信息

Booij J, Knol R J, Reneman L, de Bruin K, Janssen A G, van Royen E A

机构信息

Graduate School of Neurosciences, Department of Nuclear Medicine, Academic Medical Center, University of Amsterdam, The Netherlands.

出版信息

Eur J Nucl Med. 1998 Dec;25(12):1666-9. doi: 10.1007/s002590050346.

DOI:10.1007/s002590050346

PMID:9871099

Abstract

Iodine-123 labelled 2beta-carbomethoxy-3beta-4-iodophenylnortropane (nor-beta-CIT), a radioiodinated cocaine analogue, was evaluated as an agent for the in vivo labelling of serotonin transporters by biodistribution studies in rats. Intravenous injection of [123I]nor-beta-CIT resulted in high accumulation of radioactivity in brain areas with high densities of serotonin (hypothalamus) and dopamine transporters (striatum), although the binding was less pronounced in the hypothalamus. While binding of [123I]nor-beta-CIT in the hypothalamus was blocked significantly by fluvoxamine (a selective serotonin transporter blocker) but not by GBR12,909 (a selective dopamine transporter blocker), the opposite was observed in the striatum. The results of this study indicate that [123I]nor-beta-CIT, although not being a selective radioligand, binds specifically to serotonin transporters in the hypothalamus in vivo and thus suggest that [123I]nor-beta-CIT promises to be a suitable radioligand for single-photon emission tomography imaging of serotonin transporters in humans.

摘要

碘-123标记的2β-甲氧基羰基-3β-（4-碘苯基）去甲托烷（nor-β-CIT），一种放射性碘化可卡因类似物，通过在大鼠体内的生物分布研究，被评估为一种用于体内标记5-羟色胺转运体的试剂。静脉注射[123I]nor-β-CIT导致放射性在5-羟色胺（下丘脑）和多巴胺转运体（纹状体）高密度的脑区中高度蓄积，尽管在下丘脑中的结合不太明显。虽然氟伏沙明（一种选择性5-羟色胺转运体阻滞剂）可显著阻断[123I]nor-β-CIT在下丘脑中的结合，但GBR12,909（一种选择性多巴胺转运体阻滞剂）则不能，而在纹状体中观察到的情况则相反。这项研究的结果表明，[123I]nor-β-CIT虽然不是一种选择性放射性配体，但在体内可特异性结合下丘脑中的5-羟色胺转运体，因此表明[123I]nor-β-CIT有望成为一种适用于人类5-羟色胺转运体单光子发射断层扫描成像的放射性配体。