Labeling cyclic glycoprotein IIb/IIIa receptor antagonists with Tc-99m by the preformed chelate approach: Effects of chelators on properties of [Tc-99m]chelator-peptide conjugates

被引：85

作者：

Liu, S

Edwards, DS

Looby, RJ

Poirier, MJ

Rajopadhye, M

Bourque, JP

Carroll, TR

机构：

[1] Radiopharmaceuticals Division, DuPont Merck Pharmaceutical Company, North Billerica, MA 01862

来源：

BIOCONJUGATE CHEMISTRY | 1996年 / 7卷 / 02期

关键词：

D O I：

10.1021/bc9500958

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Several cyclic GPIIb/IIIa receptor antagonists were labeled with Tc-99m by the preformed chelate approach using chelators such as H(4)L1 [4,5-bis(mercaptoacetamido)pentanoic acid], H(4)L2 [3,4-bis-(mercaptoacetamido)benzoic acid], H(3)L3 [2-(mercapto)ethylaminoacetyl-L-cysteine], H(4)L4 [N-(mercaptoacetyl)glycylglycylglycine], H(4)L5 [N-[2-(mercapto)propionyl]glycylglycylglycine], and H(4)L6 [N-[2-(mercapto)propionyl]glycylglycyl-gamma-aminobutyric acid]. In this approach, the [Tc-99m]chelator complexes are formed first, followed by the activation of the carboxylic group on the complex by formation of its tetrafluorophenol (TFP) ester and the conjugation of the TFP ester with an amino group of a cyclic GPIIb/IIIa receptor antagonist. The Tc-99m-labeled cyclic GPIIb/IIIa receptor antagonists were characterized by radio-HPLC (high-performance liquid chromatography); differences in lipophilicity of the [Tc-99m]chelator-peptide conjugate are attributable to the effects of both the cyclic peptide and the chelator.

引用

页码：196 / 202

页数：7

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