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Responsive MR-imaging probes for N-methyl-D-aspartate receptors and direct visualisation of the cell-surface receptors by optical microscopy

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Gottschalk,  S
Department High-Field Magnetic Resonance, Max Planck Institute for Biological Cybernetics, Max Planck Society;
Max Planck Institute for Biological Cybernetics, Max Planck Society;

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Engelmann,  J
Department High-Field Magnetic Resonance, Max Planck Institute for Biological Cybernetics, Max Planck Society;
Max Planck Institute for Biological Cybernetics, Max Planck Society;

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Citation

Sim, N., Gottschalk, S., Pal, R., Engelmann, J., Parker, D., & Mishra, A. (2013). Responsive MR-imaging probes for N-methyl-D-aspartate receptors and direct visualisation of the cell-surface receptors by optical microscopy. Chemical Science, 4(8), 3148-3153. doi:10.1039/C3SC50903F.


Cite as: http://hdl.handle.net/11858/00-001M-0000-001A-136B-5
Abstract
A series of N-methyl-D-aspartate (NMDA) receptor-targeted MRI contrast agents has been developed, based on the known competitive NMDA antagonist, 3,4-diamino-3-cyclobutene-1,2-dione. Their use as responsive MR imaging probes has been evaluated in vitro and two contrast agents showed 170–176 enhancements in relaxation rate, following incubation with a neuronal cell line model. A derivative of the lead compound was prepared containing a biotin moiety, and both the specificity and reversibility of binding to the NMDA cell surface receptors demonstrated using confocal microscopy.