Synthesis and 124I-labeling of m-iodophenylpyrrolomorphinan as a potential PET imaging agent for delta opioid (DOP) receptors

被引：6

作者：

Akgun, Eyup ^{[1
]}

Portoghese, Philip S.

Sajjad, Munawwar

Nabi, Hani A.

机构：

[1] Univ Minnesota, Coll Pharm, Dept Med Chem, Minneapolis, MN 55455 USA

[2] SUNY Buffalo, Dept Nucl Med, Buffalo, NY 14214 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2007年 / 50卷 / 3-4期

关键词：

m-IPPM; DOP receptor agonist; iodine-124; positron emission tomography;

D O I：

10.1002/jlcr.1216

中图分类号：

Q5 [生物化学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Condensation of phenylazo-beta-ketoamide 4 with oxymorphone 5 afforded an m-iodophenylpyrrolomorphinan (m-IPPM) 6 mediated by elemental zinc in acetic acid/sodium acetate buffer. m-IPPM 6 is a novel opioid receptor agonist (K-i = 4.53 nM for DOP) with high selectivity for DOP receptors. m-IPPM 6 was converted into the positron emitter m-[I-124]PPM 8 via the stannylated intermediate 7. The final yield was 24.5 +/- 1.9 % (n = 6) with a specific activity of 2.5 +/- 1.2 Ci/mu mol. Copyright (C) 2007 John Wiley & Sons, Ltd.

引用

页码：165 / 170

页数：6

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