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Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate on the binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate studied by autoradiography in rat forebrain.
Neurochem Int. 1995 Feb; 26(2):155-64.NI

Abstract

L-trans-Pyrrolidine-2,4-dicarboxylate (L-t-PDC) and L-threo-3- hydroxyaspartate (L-t-3OHA), compounds known to interact strongly with the Na(+)-dependent high affinity uptake of excitatory amino acids in central nervous tissue, were tested as potential inhibitors of binding to glutamate receptors and transport sites in frozen sections of rat brain. [3H] alpha-amino-3-hydroxy- 5-methyl-4-isoxazolepropionate (AMPA), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), and [3H] kainate were used as ligands for the binding sites on the "non-NMDA" classes of glutamate receptors and [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653) was used to label NMDA receptor binding sites. The Na(+)-dependent glutamate-uptake site was marked by [3H]L-aspartate. The autoradiograms, obtained by exposing 3H-sensitive film to sections of rat forebrain preincubated with 3H-labelled ligands, were scanned by laser beam and quantified. Distribution patterns of the receptor and transporter sites visualized by the 3H-labelled ligands were compatible with previously published results. [3H]CNQX binding, however, was found to be significantly decreased by Na+.L-t-3OHA was about an order of magnitude stronger than L-t-PDC as an inhibitor of [3H]L-aspartate binding. Neither of the compounds had any important effect at the "non-NMDA" receptor binding sites but L-t-3OHA was a weak inhibitor of [3H]CGP 39653 binding (< 40% at 100 microM). The results suggest that, at low nanomolar concentrations, both compounds are likely to be selective for Na(+)-dependent high affinity glutamate transporter sites. Moreover, L-t-3OHA seems to have a sufficiently high affinity for the site to be almost certainly useful, if available in a 3H-labelled form, as a ligand in autoradiographic studies.

Authors+Show Affiliations

Department of Anatomy and Histology, University of Sydney, NSW, Australia.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

7541266

Citation

Balcar, V J., et al. "Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate On the Binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate Studied By Autoradiography in Rat Forebrain." Neurochemistry International, vol. 26, no. 2, 1995, pp. 155-64.
Balcar VJ, Li Y, Killinger S. Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate on the binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate studied by autoradiography in rat forebrain. Neurochem Int. 1995;26(2):155-64.
Balcar, V. J., Li, Y., & Killinger, S. (1995). Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate on the binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate studied by autoradiography in rat forebrain. Neurochemistry International, 26(2), 155-64.
Balcar VJ, Li Y, Killinger S. Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate On the Binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate Studied By Autoradiography in Rat Forebrain. Neurochem Int. 1995;26(2):155-64. PubMed PMID: 7541266.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of L-trans-pyrrolidine-2,4-dicarboxylate and L-threo-3-hydroxyaspartate on the binding of [3H]L-aspartate, [3H]alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA), [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and [3H]kainate studied by autoradiography in rat forebrain. AU - Balcar,V J, AU - Li,Y, AU - Killinger,S, PY - 1995/2/1/pubmed PY - 1995/2/1/medline PY - 1995/2/1/entrez SP - 155 EP - 64 JF - Neurochemistry international JO - Neurochem Int VL - 26 IS - 2 N2 - L-trans-Pyrrolidine-2,4-dicarboxylate (L-t-PDC) and L-threo-3- hydroxyaspartate (L-t-3OHA), compounds known to interact strongly with the Na(+)-dependent high affinity uptake of excitatory amino acids in central nervous tissue, were tested as potential inhibitors of binding to glutamate receptors and transport sites in frozen sections of rat brain. [3H] alpha-amino-3-hydroxy- 5-methyl-4-isoxazolepropionate (AMPA), [3H]6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), and [3H] kainate were used as ligands for the binding sites on the "non-NMDA" classes of glutamate receptors and [3H]DL-(E)-2-amino-4-propyl-5-phosphono-3-pentenoate (CGP 39653) was used to label NMDA receptor binding sites. The Na(+)-dependent glutamate-uptake site was marked by [3H]L-aspartate. The autoradiograms, obtained by exposing 3H-sensitive film to sections of rat forebrain preincubated with 3H-labelled ligands, were scanned by laser beam and quantified. Distribution patterns of the receptor and transporter sites visualized by the 3H-labelled ligands were compatible with previously published results. [3H]CNQX binding, however, was found to be significantly decreased by Na+.L-t-3OHA was about an order of magnitude stronger than L-t-PDC as an inhibitor of [3H]L-aspartate binding. Neither of the compounds had any important effect at the "non-NMDA" receptor binding sites but L-t-3OHA was a weak inhibitor of [3H]CGP 39653 binding (< 40% at 100 microM). The results suggest that, at low nanomolar concentrations, both compounds are likely to be selective for Na(+)-dependent high affinity glutamate transporter sites. Moreover, L-t-3OHA seems to have a sufficiently high affinity for the site to be almost certainly useful, if available in a 3H-labelled form, as a ligand in autoradiographic studies. SN - 0197-0186 UR - https://www.unboundmedicine.com/medline/citation/7541266/Effects_of_L_trans_pyrrolidine_24_dicarboxylate_and_L_threo_3_hydroxyaspartate_on_the_binding_of_[3H]L_aspartate_[3H]alpha_amino_3_hydroxy_5_methyl_4_isoxazolepropionate__AMPA__[3H]DL__E__2_amino_4_propyl_5_phosphono_3_pentenoate__CGP_39653__[3H]6_cyano_7_nitroquinoxaline_23_dione__CNQX__and_[3H]kainate_studied_by_autoradiography_in_rat_forebrain_ L2 - https://linkinghub.elsevier.com/retrieve/pii/019701869400120J DB - PRIME DP - Unbound Medicine ER -