Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors

被引：12

作者：

Ametamey, SM ^{[1
]}

Kokic, M

Carrey-Rémy, N

Bläuenstein, P

Willmann, M

Bischoff, S

Schmutz, M

Schubiger, PA

Auberson, YP

机构：

[1] Paul Scherrer Inst, ETH Zurich, Ctr Radiopharmaceut Sci, CH-5232 Villigen, Switzerland

[2] Univ Zurich Hosp, Div Nucl Med, CH-5232 Villigen, Switzerland

[3] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 01期

关键词：

labelling; neurologically active compounds; antagonists; anticonvulsent;

D O I：

10.1016/S0960-894X(99)00576-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(D)-7-Iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione (I-PAMQX), is a potent, in vivo active antagonist acting at the glycine binding site of the NMDA receptor complex. Radioiodinated [I-131]I-PAMQX was prepared with good yields and high specific activity from its 7-bromo analogue. Biodistribution studies of [I-131]I-PAMQX in mice showed a relatively slow clearance from the blood. The uptake of radioactivity was highest in the kidneys, moderate in the heart, lung, liver and bones, and low in the brain. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：75 / 78

页数：4

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