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Relaxometry, animal biodistribution, and magnetic resonance imaging studies of some new gadolinium (III) macrocyclic phosphinate and phosphonate monoester complexes

Authors :
István Lázár
F. Maton
A. D. Sherry
K. McMillan
P. Bogner
B. Sumegi
Carlos F. G. C. Geraldes
Attila Miseta
Ervin Berényi
R. N. Muller
G. E. Kiefer
Source :
Magnetic Resonance in Medicine. 30:696-703
Publication Year :
1993
Publisher :
Wiley, 1993.

Abstract

The Gd3+ complexes of three new phosphorus containing tetraaza macrocycles (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis (methylene ethylphosphonic acid), H4DOTEP; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis (methylene phosphonic acid monoethylester), H4DOTPME; and the corresponding n-butyl ester, H4DOTPMB) were prepared and examined for possible use as MRI contrast agents. Although thermodynamically and kinetically less stable than Gd(DOTA)- in saline and HSA solution, the stability of these new macrocyclic complexes appears to be sufficiently high for in vivo applications. NMRD relaxivity profiles of the three complexes indicate that the number of inner sphere water molecules for these chelates is < or = 1 and that the more hydrophobic chelate, Gd(DOTPMB), binds to human serum albumin (HSA). Biodistribution studies of the radioactive 153Sm or 159Gd chelates in rats, gamma imaging of the 153Sm chelates in rats, and proton MRI studies of the nonradioactive Gd3+ chelates in rabbits all indicate that the DOTPMB complexes accumulate preferentially in the liver, spleen, and small intestines while the more hydrophilic DOTEP and DOTPME complexes appear to display renal clearances similar to other low molecular weight contrast agents.

Details

ISSN :
15222594 and 07403194
Volume :
30
Database :
OpenAIRE
Journal :
Magnetic Resonance in Medicine
Accession number :
edsair.doi.dedup.....b2bbae1f1cd7180d70a70b943d57eb6b
Full Text :
https://doi.org/10.1002/mrm.1910300607