放射性碘化2'-碘螺哌隆：一种用于体内多巴胺受体研究的新型放射性配体。

Radioiodinated 2'-iodospiperone: a new radioligand for in vivo dopamine receptor study.

作者信息

Saji H, Nakatsuka I, Shiba K, Tokui T, Horiuchi K, Yoshitake A, Torizuka K, Yokoyama A

机构信息

Faculty of Pharmaceutical Sciences and School of Medicine, Kyoto University, Japan.

出版信息

Life Sci. 1987 Oct 26;41(17):1999-2006. doi: 10.1016/0024-3205(87)90473-5.

DOI:10.1016/0024-3205(87)90473-5

PMID:3669906

Abstract

In vivo dopamine receptor binding of the newly synthesized ligand, 125I-2'-iodospiperone (125I-2'-ISP), was studied in mouse brain. The highest accumulation was found in the striatum. Analysis of the striatal homogenate showed the 125I-2'-ISP to be metabolically stable. Furthermore, this striatal binding was saturable and displaced only by dopaminergic drugs. On the other hand, the accumulation in the cortex was as low as that of the cerebellum and uneffected by the administration of serotoninergic drugs and dopaminergic drugs; results assessed by macroautoradiographic studies. Thus, the newly synthesized 125I-2'-ISP presented high affinity for dopamine receptors in vivo and therefore, holds great potential for the in vivo dopamine receptor studies, provided 123I becomes readily available.

摘要

在小鼠脑中研究了新合成配体125I-2'-碘螺哌隆（125I-2'-ISP）的体内多巴胺受体结合情况。发现纹状体中的积累量最高。纹状体匀浆分析表明125I-2'-ISP在代谢上是稳定的。此外，这种纹状体结合是可饱和的，并且仅被多巴胺能药物取代。另一方面，皮层中的积累量与小脑一样低，并且不受血清素能药物和多巴胺能药物给药的影响；通过宏观放射自显影研究评估结果。因此，新合成的125I-2'-ISP在体内对多巴胺受体具有高亲和力，因此，如果123I容易获得，在体内多巴胺受体研究中具有很大潜力。