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

Content Provider	Springer Nature Link
Author	Zigelboim, Isaac Offen, Daniel Melamed, Eldad Panet, Hana Rehavi, Moshe Cohen, Yoram
Copyright Year	2007
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 R$_{1}$ 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 R$_{2}$ 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.
Starting Page	323
Ending Page	329
Page Count	7
File Format	PDF
ISSN	09230750
Journal	Journal of Inclusion Phenomena and Macrocyclic Chemistry
Volume Number	59
Issue Number	3-4
e-ISSN	15731111
Language	English
Publisher	Springer Netherlands
Publisher Date	2007-07-24
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Dopamine receptor Gadolinium complexes MRI contrast agents MR molecular imaging Targeted contrast agents Crystallography Food Science Organic Chemistry
Content Type	Text
Resource Type	Article
Subject	Chemistry Condensed Matter Physics Food Science

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