N1′-(p-[18F]fluorobenzyl)naltrindole (p-[18F]BNTI) as a potential PET imaging agent for DOP receptors

被引：9

作者：

Akgun, Eyup ^{[1
]}

Sajjad, Munawwar

Portoghese, Philip S.

机构：

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

[2] Univ Minnesota, Dept Radiol, Sch Med, Minneapolis, MN 55455 USA

[3] VAMC, PET Imaging Serv, Minneapolis, MN 55417 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2006年 / 49卷 / 10期

关键词：

FBNTI; delta opioid receptors; fluorine-18; positron emission tomography;

D O I：

10.1002/jlcr.1095

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：

The N1'-(p-fluorobenzyl)naltrindole 5 has been synthesized by reaction of 3-O-benzyl NTI 3 with p-fluorobenzylbromide under phase transfer catalysis. The subsequent 3-O-benzyldeprotection of 4 in HBr/CH3COOH gave the target compound 5 in three steps from naltrindole 2. p-FBNTI 5 is a novel delta opioid receptor antagonist (K-i=0.00312 nM) and antagonizes the delta opioid (DOP) agonist, DPDPE, with a K-e = 1.55 nM in the mouse vas deferens preparation. Using the same synthetic strategy the synthesis of p-[F-18]BNTI 10 was undertaken. The final yield was 4% and the specific activity varied in a range of 250-400 mCi/pmol. Copyright (c) 2006 John Wiley & Sons, Ltd.

引用

页码：857 / 866

页数：10

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