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用于与血浆蛋白进行体内非共价络合的钆(III)二螯合物和四螯合物:血池磁共振成像造影剂的一种新型分子设计

Gadolinium(III) di- and tetrachelates designed for in vivo noncovalent complexation with plasma proteins: a novel molecular design for blood pool MRI contrast enhancing agents.

作者信息

Martin V V, Ralston W H, Hynes M R, Keana J F

机构信息

Department of Chemistry, University of Oregon, Eugene 97403, USA.

出版信息

Bioconjug Chem. 1995 Sep-Oct;6(5):616-23. doi: 10.1021/bc00035a017.

DOI:10.1021/bc00035a017
PMID:8974462
Abstract

A new series of gadolinium chelates designed as blood pool contrast enhancing agents for magnetic resonance imaging applications is described. Complexes having four Gd(III) chelate units display a significant increase in molecular relaxivity per gadolinium ion in water (9-13 L x mmol(-1) x (s-1) compared to Gd(III)-DTPA (5 L x mmol(-1) x s(-1). A further jump in relaxivity (25 L x mmol(-1) x sec(-1) in 4% BSA solution was observed in the case of a fatty acid-containing tetrachelate and is attributed to noncovalent binding of the tetrachelate to serum albumin. This agent was successfully used for imaging the rat circulatory system.

摘要

本文描述了一系列新的钆螯合物,它们被设计用作磁共振成像应用中的血池造影剂。具有四个钆(III)螯合单元的配合物在水中每个钆离子的分子弛豫率显著增加(9 - 13 L·mmol⁻¹·s⁻¹),相比之下钆(III)-二乙三胺五乙酸(Gd(III)-DTPA)为5 L·mmol⁻¹·s⁻¹。在含脂肪酸的四螯合物的情况下,在4%牛血清白蛋白溶液中弛豫率进一步跃升(25 L·mmol⁻¹·sec⁻¹),这归因于四螯合物与血清白蛋白的非共价结合。该造影剂已成功用于大鼠循环系统成像。

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