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Sim, N.* ; Pal, R.* ; Parker, D.J.* ; 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.

Org. Biomol. Chem. 12, 9389-9404 (2014)
DOI
Open Access Green as soon as Postprint is submitted to ZB.
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.
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Publication type Article: Journal article
Document type Scientific Article
ISSN (print) / ISBN 1477-0520
e-ISSN 1477-0539
Journal Organic & Biomolecular Chemistry
Quellenangaben Volume: 12, Issue: 46, Pages: 9389-9404 Article Number: , Supplement: ,
Publisher Royal Society of Chemistry (RSC)
Reviewing status Peer reviewed
Institute(s) Institute of Biological and Medical Imaging (IBMI)