Densely packed Gd(III)-chelates with fast water exchange on a calix[4]arene scaffold: a potential MRI contrast agent

Daniel T. Schuhle, Miloslav Polasek, Ivan Lukes, Thomas Chauvin, Eva Toth, Juergen Schatz, Ulf Hanefeld, Marc C. A. Stuart, Joop A. Peters*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

24 Citations (Scopus)

Abstract

A pyridine-N-oxide functionalized DOTA analogue has been conjugated to a calix[4]arene and the corresponding Gd-complex was characterized with respect to its suitability as MRI contrast agent. The compound forms spherical micelles in water with a cmc of 35 mu M and a radius of 8.2 nm. The relaxivity of these aggregates is 31.2 s(-1) mM(-1) at 25 degrees C and 20 MHz, which corresponds to a molecular relaxivity of 125 s(-1) mM(-1). The high relaxivity mainly originates from the short tau(M) (72.7 ns) and the size of the micelles. The interaction with bovine serum albumin (BSA) was studied and an observed relaxivity of up to 40.8 s(-1) mM(-1) (163.2 s(-1) mM(-1) per binding place) at 20 MHz and 37 degrees C was found in the presence of 2.0 mM protein.

Original languageEnglish
Pages (from-to)185-191
Number of pages7
JournalDalton Transactions
Volume39
Issue number1
DOIs
Publication statusPublished - 2010

Keywords

  • N-OXIDE ANALOGS
  • LANTHANIDE(III) COMPLEXES
  • HIGH RELAXIVITY
  • SERUM-ALBUMIN
  • DOTA
  • NMR
  • SENSITIVITY
  • ISOMER

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