Displacement of excitatory amino acid receptor ligands by acidic oligopeptides |
| |
Authors: | V Varga R Janáky K -M Marnela J Gulyás P Kontro S S Oja |
| |
Institution: | (1) Tampere Brain Research Center, Department of Biomedical Sciences, University of Tampere, Box 607, SF-33101 Tampere, Finland;(2) Department of Chemistry, Eötvös Lorand University, H-1088 Budapest, Hungary |
| |
Abstract: | A number ofD-glutamyl andL-aspartyl dipeptides, glutathione, -D-glutamylglycine and -D-glutamyltaurine, were tested for their efficacy to displace ligands specific for different subtypes of excitatory amino acid receptors from rat brain synaptic membranes. In general, theL enanthiomorphs of -glutamyl peptides were more potent displacers than -D-glutamylglycine and-taurine but the latter were more specific for the quisqualate type of receptors. -L-glutamyl-L-glutamate was the most effective dipeptide in displacing the binding of glutamate, 2-amino-3-hydroxy-5-methylisoxazole-4-proprionate (AMPA) and 2-amino-5-phosphonoheptanoate (APH), whereas -L-glutamyl-L-aspartate was the most effective in the binding of kainate. Both oxidized and reduced glutathione were inhibitory, being most potent in the binding of AMPA. -L-Glutamylaminomethylsulphonate was most effective in the binding of APH. The most potent -L-glutamyl peptides (glutathione, -L-glutamyl-L-glutamate,-L-aspartate, and-glycine) may act as endogenous modulators of excitatory aminoacidergic neurotransmission. |
| |
Keywords: | Neurotransmission excitatory amino acids receptors ligand binding glutamyl peptides |
本文献已被 SpringerLink 等数据库收录! |
|