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Bioconjug Chem. 2012 Jan 18;23(1):21-6. doi: 10.1021/bc100571g. Epub 2011 Dec 13.

Confocal microscopy imaging of NR2B-containing NMDA receptors based on fluorescent ifenprodil-like conjugates.

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CNRS UMR6232, Université de Caen-Basse Normandie, Cyceron, Boulevard Henri Becquerel, Caen Cedex, France.


We describe the synthesis and pharmacological characterization of a first generation of ifenprodil conjugates 4-7 as fluorescent probes for the confocal microscopy imaging of the NR2B-containing NMDA receptor. The fluorescein conjugate 6 displayed a moderate affinity for NMDAR but a high selectivity for the NR2B subunit and its NTD. Fluorescence imaging of DS-red labeled cortical neurons showed an exact colocalization of the probe 6 with small protrusions along the dendrites related to a specific binding on NR2B-containing NMDARs.

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