A novel fluorescent GSH-adduct binds to the NMDA receptor.
In an attempt to develop various fluorescent probes to label glutathione (GSH) receptors, we have serendipitously synthesized a probe that binds to and antagonizes the NMDA receptor. Probe 1, a GSH adduct, displaces the competitive NMDA antagonist [3H]-CGP 39653 with a higher affinity than NMDA or cysteine in rat synaptic membranes. In recording experiments from a rat cortical 'wedge' preparation, Probe 1 reversibly blocks both NMDA- and cysteine-induced depolarization. In mixed astrocyte-neuron tissue culture preparations, Probe 1 labels parts of both cell bodies as well as processes. The present data suggest that Probe 1 binds to the NMDA receptor and antagonizes channel function.
Shaw
C A
CA
Department of Ophthalmology, c/o Department of Anatomy, University of British Columbia, Vancouver, Canada. cshaw@interchange.ubc.ca
Pasqualotto
B A
BA
Curry
K
K
Kim
S U
SU
LeCompte
K A
KA
Langmuir
M E
ME
D015763:2-Amino-5-phosphonovalerate / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D002478:Cells, Cultured; D018691:Excitatory Amino Acid Antagonists / Q000378:metabolism; D005333:Fetus; D005456:Fluorescent Dyes / Q000378:metabolism*; D006801:Humans; D009457:Neuroglia; D009474:Neurons; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D018000:Receptors, Peptide / Q000378:metabolism*
D018691:Excitatory Amino Acid Antagonists; D005456:Fluorescent Dyes; D016194:Receptors, N-Methyl-D-Aspartate; D018000:Receptors, Peptide; C035560:glutathione receptor; C069052:CGP 39653; D015763:2-Amino-5-phosphonovalerate