[11C] - 和 [125I]IMB 的制备：一种多巴胺 D - 2 受体拮抗剂。

Preparation of [11C]- and [125I]IMB: a dopamine D-2 receptor antagonist.

作者信息

Wilson A A, Dannals R F, Ravert H T, Wagner H N

机构信息

Division of Nuclear Medicine, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.

出版信息

Int J Rad Appl Instrum A. 1989;40(5):369-73. doi: 10.1016/0883-2889(89)90199-8.

DOI:10.1016/0883-2889(89)90199-8

PMID:2548972

Abstract

A new dopamine D-2 receptor ligand, N-[2-(N'-4-iodobenzyl-N'-methyl)aminoethyl]-5-chloro-2-methoxy-4- (methylamino)benzamide (IMB) was synthesized and labelled with 11C and 125I at high specific activities. Both radiotracers were prepared by alkylation reactions with [11C]iodomethane and [125I]4-iodobenzyl bromide and appropriate 2 degrees amine precursors. Isolated radiochemical yields of 12-20% for [11C]IMB and 35-50% for [125I]IMB were achieved in 24 and 130-150 min respectively. [11C]IMB and [123I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.

摘要

一种新的多巴胺D-2受体配体，N-[2-(N'-4-碘苄基-N'-甲基)氨基乙基]-5-氯-2-甲氧基-4-(甲氨基)苯甲酰胺(IMB)被合成，并以高比活度用11C和125I进行标记。两种放射性示踪剂均通过与[11C]碘甲烷和[125I]4-碘苄基溴以及合适的仲胺前体进行烷基化反应制备。[11C]IMB的放射性化学产率在24分钟内达到12-20%，[125I]IMB的放射性化学产率在130-150分钟内达到35-50%。[11C]IMB和[123I]IMB可能适用于在神经受体定位和定量方面对PET和SPECT进行直接比较。