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

Neil Sim; Sven Gottschalk; Robert Pal; Jörn Engelmann; David Parker; Anurag Mishra

doi:10.1039/c3sc50903f

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

Neil Sim, Sven Gottschalk, Robert Pal, Jörn Engelmann, David Parker^*, Anurag Mishra^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

14 Citations (Scopus)

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.

Original language	English
Pages (from-to)	3148-3153
Number of pages	6
Journal	Chemical Science
Volume	4
Issue number	8
Early online date	6 Jun 2013
DOIs	https://doi.org/10.1039/c3sc50903f
Publication status	Published - 1 Aug 2013

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

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.",

author = "Neil Sim and Sven Gottschalk and Robert Pal and J{\"o}rn Engelmann and David Parker and Anurag Mishra",

note = "We thank the EPSRC and the ERC (FCC266804) for support. Publisher Copyright: {\textcopyright} The Royal Society of Chemistry 2013",

year = "2013",

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doi = "10.1039/c3sc50903f",

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T1 - Responsive MR-imaging probes for N-methyl-d-aspartate receptors and direct visualisation of the cell-surface receptors by optical microscopy

AU - Sim, Neil

AU - Gottschalk, Sven

AU - Pal, Robert

AU - Engelmann, Jörn

AU - Parker, David

AU - Mishra, Anurag

PY - 2013/8/1

Y1 - 2013/8/1

N2 - 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.

AB - 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.

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DO - 10.1039/c3sc50903f

M3 - Journal article

AN - SCOPUS:84880003865

SN - 2041-6520

VL - 4

SP - 3148

EP - 3153

JO - Chemical Science

JF - Chemical Science

IS - 8

ER -

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

Abstract

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