碘乙基螺哌隆，一种用于探索中枢多巴胺D2受体的新型潜在药物：合成及初步体内研究。

Iodoethylspiperone, a new potential agent for exploration of central dopamine D2 receptors: synthesis and preliminary in vivo study.

作者信息

Chalon S, Frangin Y, Guilloteau D, Caillet M, Guimbal C, Schmitt M H, Desplanches G, Baulieu J L, Besnard J C

机构信息

INSERM U316, Laboratoire de Biophysique Médicale, Tours, France.

出版信息

Int J Rad Appl Instrum B. 1990;17(4):389-95. doi: 10.1016/0883-2897(90)90106-b.

DOI:10.1016/0883-2897(90)90106-b

PMID:2143754

Abstract

We synthesized a new spiperone derivative: iodoethylspiperone (IES) to perform dopamine D2 receptor exploration by SPECT. IES was prepared from a precursor: tosylethylspiperone, and characterized by i.r. and 1H-NMR analyses. [125I]IES was obtained with 80% yield. In vivo biodistribution in rats showed a high and specific uptake in the striatum. The uptake ratio between the striatum and the cerebellum reached a maximum value 4 h after injection (10.05 +/- 2.81). IES labeled with 123I should be a promising new agent to investigate D2 receptors in the living human brain.

摘要

我们合成了一种新的螺哌隆衍生物

碘乙基螺哌隆（IES），用于通过单光子发射计算机断层扫描（SPECT）进行多巴胺D2受体研究。IES由前体对甲苯磺酰乙基螺哌隆制备，并通过红外光谱（i.r.）和核磁共振氢谱（1H-NMR）分析进行表征。[125I]IES的产率为80%。大鼠体内生物分布显示纹状体有高特异性摄取。注射后4小时纹状体与小脑的摄取比达到最大值（10.05±2.81）。用123I标记的IES应该是一种有前景的新型药物，可用于在活体人脑中研究D2受体。