一种用于绘制阿片受体的放射性碘化7α-O-碘代烯丙基二丙诺啡。

A radioiodinated 7alpha-O-iodoallyl diprenorphine for mapping opioid receptors.

作者信息

Wang R F, Tafani J A, Zajac J M, Guiraud R

机构信息

Department of Nuclear Medicine, The First Hospital, Beijing Medical University, Beijing, P.R. of China.

出版信息

Neuropeptides. 1999 Dec;33(6):498-502. doi: 10.1054/npep.1999.0769.

DOI:10.1054/npep.1999.0769

PMID:10657531

Abstract

The aim of the current research has been to validate an original radioiodinated diprenorphine (DPN) derivative suitable for imaging studies of opioid receptors. [(125)I]7alpha-O-iodoallyl diprenorphine (7alpha-O-IA-DPN) was prepared by radioiododestannylation and in vitro and in vivo opioid receptor binding assays were performed with CDF1 mouse brains. In vitro binding studies showed high affinity (K(i)= 0.4 +/- 0.2 nM) for mouse brain membranes. In vivo studies showed 63% specific binding. Ex vivo autoradiography of brain sections confirmed high uptake and retention of [(125)I]7alpha-O-IA-DPN in regions rich in opioid receptors. This new radioiodinated DPN analogue appears to be a potential radioprobe for in vivo visualization of human cerebral opioid receptors with single photon emission computed tomography (SPECT).

摘要

当前研究的目的是验证一种适用于阿片受体成像研究的新型放射性碘化二丙诺啡（DPN）衍生物。通过放射性碘脱锡反应制备了[(125)I]7α-O-碘烯丙基二丙诺啡（7α-O-IA-DPN），并使用CDF1小鼠脑进行了体外和体内阿片受体结合试验。体外结合研究表明其对小鼠脑膜具有高亲和力（K(i)= 0.4 +/- 0.2 nM）。体内研究显示特异性结合率为63%。脑切片的离体放射自显影证实[(125)I]7α-O-IA-DPN在富含阿片受体的区域有高摄取和滞留。这种新型放射性碘化DPN类似物似乎是一种潜在的放射性探针，可用于通过单光子发射计算机断层扫描（SPECT）对人脑阿片受体进行体内可视化。