HEPATOBILIARY AND RENAL EXCRETION IN MICE OF CHARGED AND NEUTRAL GADOLINIUM COMPLEXES OF CYCLIC TETRA-AZA-PHOSPHINIC AND CARBOXYLIC-ACIDS

被引:51
作者
HARRISON, A
WALKER, CA
PEREIRA, KA
PARKER, D
ROYLE, L
PULUKKODY, K
NORMAN, TJ
机构
[1] Medical Research Council, Radiobiology Unit, Chilton
[2] Department of Chemistry, University of Durham, Durham, DH1 3LE, South Road
关键词
GADOLINIUM; MRI CONTRAST AGENTS; CYCLIC LIGANDS; BIODISTRIBUTION; HEPATOBILIARY;
D O I
10.1016/0730-725X(93)90194-I
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
Tissue distribution of 21 new Gd-157/153 complexes was measured at 5 min and 24 hr after an intravenous injection into mice. A complex was judged to be stable in vivo when the percentage of Gd-153 retained in the liver and skeleton at 24 hr was comparable with that of Gd-153(DOTA)-. Complexes varied in net charge and lipophilicity and 20 were phosphinic or carboxylic acid derivatives of tetra-aza-cyclo-dodecane. Three anionic, lipophilic complexes were cleared predominantly by the hepato-biliary pathway and were stable in vivo. The remaining 18 complexes were cleared mainly by the kidneys. Of these 18, 1 anionic, 8 neutral, and 3 cationic complexes were stable in vivo. These findings augur well for the future of hepato-biliary and general purpose Gd contrast enhancing agents for MRI.
引用
收藏
页码:761 / 770
页数:10
相关论文
共 14 条
[1]  
Runge, Bradley, Et al., Clinical safety and efficacy of gadoteridol: A study in 411 patients with suspected intracranial and spinal disease, Radiology, 181, pp. 701-709, (1991)
[2]  
Chang, Kumar, Garrison, Brittain, Tweedle, Physico-chemical properties of Gd(HP-DO3A): A nonionic, macrocyclic magnetic resonance imaging contrast agent, Book of Abstracts: Ninth Annual Meeting of the Society of Magnetic Resonance in Medicine, (1990)
[3]  
Pavone, Parrizio, Buoni, Tettamanti, Passariello, Musu, Tirone, Felder, Comparison of Gd-BOPTA with Gd-DTPA in MR imaging of rat liver, Radiology, 176, pp. 61-64, (1990)
[4]  
Cavagna, Dapra, Maggioni, de Haen, Felder, Gd-BOPTA/Dimeg: Experimental disease imaging, Magn. Reson. Med., 22, pp. 329-333, (1991)
[5]  
Davies, de Haen, Gadobenic acid dimeglumine salt, Drugs of the Future, 16, 11, pp. 1001-1003, (1991)
[6]  
Weinmann, Schuhmann-Giampieri, Schmitt-Willich, Vogler, Frenzel, Gries, A new lipophilic gadolinium chelate as a tissue-specific contrast medium for MRI, Magn. Reson. Med., 22, pp. 233-237, (1991)
[7]  
Parker, Pulukkody, Norman, Harrison, Royle, Walker, Stable anionic, neutral and cationic complexes of gadolinium with functionalised amino-phosphinic acid macrocyclic ligands, Journal of the Chemical Society, Chemical Communications, pp. 1441-1443, (1992)
[8]  
Pulukkody, Norman, Parker, Royle, Broan, Synthesis of charged and uncharged complexes of gadolinium and yttrium with cyclic polyazaphosphinic acid ligands for in vivo applications, Journal of the Chemical Society, Perkin Transactions 2, 2, pp. 605-620, (1993)
[9]  
Cox, Jankowski, Kataky, Parker, Beeley, Boyce, Eaton, Millar, Millican, Harrison, Walker, Synthesis of a kinetically stable yttrium-90 labelled macrocycle?antibody conjugate, Journal of the Chemical Society, Chemical Communications, 10, pp. 797-798, (1989)
[10]  
Broan, Cox, Craig, Kataky, Parker, Harrison, Randall, Ferguson, Structure and solution stability of indium and gallium complexes of 1,4,7-triazacyclononanetriacetate and of yttrium complexes of 1,4,7,10-tetraazacyclododecanetetraacetate and related ligands: kinetically stable complexes for use in imaging and radioimmunotherapy. X-Ray molecular structure of the indium and gallium complexes of 1,4,7-triazacyclononane-1,4,7-triacetic acid, Journal of the Chemical Society, Perkin Transactions 2, 2,