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

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

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cells, Cultured
  • Fluorescent Dyes / analysis*
  • Fluorescent Dyes / chemistry*
  • HEK293 Cells
  • Humans
  • Microscopy, Confocal
  • Molecular Structure
  • Piperidines / analysis*
  • Piperidines / chemistry*
  • Receptors, N-Methyl-D-Aspartate / analysis*
  • Receptors, N-Methyl-D-Aspartate / chemistry*
  • Stereoisomerism

Substances

  • Fluorescent Dyes
  • NR2B NMDA receptor
  • Piperidines
  • Receptors, N-Methyl-D-Aspartate
  • ifenprodil