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Magnetic resonance and optical imaging probes for NMDA receptors on the cell surface of neurons: synthesis and evaluation in cellulo

Sim, N.; Pal, R.; Parker, D.; Engelmann, J.; Mishra, A.; Gottschalk, S.

Magnetic resonance and optical imaging probes for NMDA receptors on the cell surface of neurons: synthesis and evaluation in cellulo Thumbnail


Authors

N. Sim

J. Engelmann

A. Mishra

S. Gottschalk



Abstract

A second generation of N-methyl-D-aspartate (NMDA) receptor-targeted MRI contrast agents has been synthesised and evaluated in cellulo, based on established bicyclic NMDA receptor antagonists. Their use as responsive MR imaging probes has been evaluated in suspensions of NSC-34 cells, and one agent exhibited significant enhancements in measured longitudinal and transverse water proton relaxation rates (19 and 38% respectively; 3 T, 298 K). A biotin derivative of the lead compound was prepared and the specificity and reversibility of binding to the NMDA cell surface receptors demonstrated using confocal laser scanning microscopy. Competitive and reversible binding of glutamate to the receptors was also visualised, suggesting that the receptor-targeted approach may allow MRI to be used to monitor neuronal events associated with modulation of local glutamate concentrations.

Citation

Sim, N., Pal, R., Parker, D., Engelmann, J., Mishra, A., & Gottschalk, S. (2014). Magnetic resonance and optical imaging probes for NMDA receptors on the cell surface of neurons: synthesis and evaluation in cellulo. Organic and Biomolecular Chemistry, 12(46), 9389-9404. https://doi.org/10.1039/c4ob01848f

Journal Article Type Article
Acceptance Date Oct 8, 2014
Online Publication Date Oct 8, 2014
Publication Date Dec 14, 2014
Deposit Date Nov 14, 2014
Publicly Available Date Nov 19, 2014
Journal Organic and Biomolecular Chemistry
Print ISSN 1477-0520
Electronic ISSN 1477-0539
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Volume 12
Issue 46
Pages 9389-9404
DOI https://doi.org/10.1039/c4ob01848f

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