用于基于多巴胺 D-1 受体的单光子发射计算机断层扫描成像的高效比活度[123I]SCH 23982 的放射性合成。

Radiosynthesis of high effective specific-activity [123I]SCH 23982 for dopamine D-1 receptor-based SPECT imaging.

作者信息

Moerlein S M, Parkinson D, Welch M J

机构信息

Edward Mallinckrodt Institute of Radiology, Washington University, St Louis, MO 63110.

出版信息

Int J Rad Appl Instrum A. 1990;41(4):381-5. doi: 10.1016/0883-2889(90)90147-9.

DOI:10.1016/0883-2889(90)90147-9

PMID:2158956

Abstract

The high yield, high-specific activity radiosynthesis of the dopaminergic D-1 receptor-binding ligand [123I]SCH 23982 is described. Using no-carrier-added iododeprotonation of the des-iodo precursor SKF 83692 and column-switching HPLC, [123I]SCH 23982 was isolated in 35-40% radiochemical yield with an effective specific activity of 2250-4000 Ci/mmol and an overall preparation time of 90 min. The procedure outlined here can be employed for the clinical production of [123I]SCH 23982 as a SPECT radiopharmaceutical, as well as [125I]SCH 23982 to be used for in vitro receptor-binding applications.

摘要

描述了多巴胺能D-1受体结合配体[123I]SCH 23982的高产率、高比活度放射性合成方法。使用无载体添加的去碘前体SKF 83692的碘去质子化反应和柱切换高效液相色谱法，以35%-40%的放射化学产率分离得到[123I]SCH 23982，有效比活度为2250-4000 Ci/mmol，总制备时间为90分钟。本文所述方法可用于临床生产作为单光子发射计算机断层扫描（SPECT）放射性药物的[123I]SCH 23982，以及用于体外受体结合应用的[125I]SCH 23982。