Issue 8, 2013
From the journal:

Chemical Science

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

Neil Sim,a   Sven Gottschalk,‡b   Robert Pal,a   Jörn Engelmann,b   David Parker*a  and  Anurag Mishra‡*a  

* Corresponding authors

a Department of Chemistry, Durham University, South Road, Durham, England
E-mail: anurag.mishra@durham.ac.uk, david.parker@durham.ac.uk
Fax: +44-191-3342051

b High Field MR Centre, Max Planck Institute for Biological Cybernetics, Spemannstrasse 41, Tuebingen, Germany

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.

Graphical abstract: 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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Article information

DOI
https://doi.org/10.1039/C3SC50903F
Article type
Edge Article
Submitted
04 ⵉⴱⵔ 2013
Accepted
05 ⵢⵓⵏ 2013
First published
06 ⵢⵓⵏ 2013

Chem. Sci., 2013,4, 3148-3153

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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

N. Sim, S. Gottschalk, R. Pal, J. Engelmann, D. Parker and A. Mishra, Chem. Sci., 2013, 4, 3148 DOI: 10.1039/C3SC50903F

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