Synthesis, binding affinity, and relaxivity of target-specific MRI contrast agents

Isaac Zigelboim, Daniel Offen, Eldad Melamed, Hana Panet, Moshe Rehavi, Yoram Cohen*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Although magnetic resonance imaging (MRI) is one of the most important imaging modalities of the central nervous system (CNS), one of the main drawbacks of MRI is its limited specificity. This can potentially be partially alleviated by target-specific contrast agents. In the present paper we describe a simple high yield synthesis of two such gadolinium-based spiperone targeted MRI contrast agents, 1a and 1b. The R1 relaxivities of 1a and 1b were evaluated and found to be 5.94 and 8.31 mM-1 s-1, respectively at 9.4T, while their R2 relaxivities at the same magnetic field were found to be 18.05 and 22.60 mM-1 s-1, respectively. In addition and very importantly compound 1a, which is a gadolinium-based, spiperone-targeted MRI contrast agent, was found to preserve some of the spiperone affinity toward the dopamine D2 receptor. Compounds 1a and 1b thus represent potential agents for in vitro dopamine receptor imaging using MRI in experimental models.

Original languageEnglish
Pages (from-to)323-329
Number of pages7
JournalJournal of Inclusion Phenomena and Macrocyclic Chemistry
Volume59
Issue number3-4
DOIs
StatePublished - Dec 2007

Keywords

  • Dopamine receptor
  • Gadolinium complexes
  • MR molecular imaging
  • MRI contrast agents
  • Targeted contrast agents

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