PREPARATION AND EVALUATION OF NEW BIFUNCTIONAL CHELATING-AGENTS - A PRELIMINARY-REPORT

被引：4
|
作者：
RICHARD, MD
THAKUR, ML
STEDMAN, J
DAMJANOV, A
DAMJANOV, I
机构：
[1] THOMAS JEFFERSON UNIV,DEPT RADIAT ONCOL,PHILADELPHIA,PA 19107
[2] THOMAS JEFFERSON UNIV,DEPT PATHOL & CELL BIOL,PHILADELPHIA,PA 19107
[3] TEMPLE UNIV,DEPT MED CHEM,PHILADELPHIA,PA 19140
来源：
NUCLEAR MEDICINE AND BIOLOGY | 1990年 / 17卷 / 02期
关键词：
D O I：
10.1016/0883-2897(90)90145-Q
中图分类号：
R8 [特种医学]; R445 [影像诊断学];
学科分类号：
1002 ; 100207 ; 1009 ;
摘要：
A scheme has been designed to synthesize a homologous series of new bifunctional chelating agents (BFCAs), which may increase the thermodynamic stability of metal chelates and conjugate at the specific sites on the monoclonal antibody molecule (MoAb) permitting us to analyze the structure-activity relationships of the series of compounds. Four such compounds have been prepared and chacterized by FT-i.r. and NMR spectroscopy. One of them has been used to label an antibody with 111In, the stability and distribution of which has been examined in tumor-bearing mice and compared to that of the 111In-MoAb prepared using cyclic anhydride of DTPA. Enhanced tumor/blood ratios (9 vs 6.5), tumour to muscle ratios (7 vs 3), and decreased liver uptake (4 vs 12%) have been obtained. © 1990.
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页码：181 / &
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