Glutamate-containing dipeptides enhance specific binding at glutamate receptors and inhibit specific binding at kainate receptors in rat brain

J. Ferkany; R. Zaczek; A. Markl; J. T. Coyle

doi:10.1016/0304-3940(84)90036-3

Glutamate-containing dipeptides enhance specific binding at glutamate receptors and inhibit specific binding at kainate receptors in rat brain

J. Ferkany, R. Zaczek, A. Markl, J. T. Coyle

School of Medicine

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

The dipeptide, l-phenylalanyl-l-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [³H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 μM with an EC₅₀ of 4.9 μM. The increase in the specific binding of [³H]AHP induced by PG results exclusively from an increase in B_max. In contrast, PG inhibits the specific binding of [³H]kainic acid to forebrain membranes with a K_i of 6.8 μM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [³H]APH and kainate receptors modulated by glutamate-containing peptides.

Original language	English (US)
Pages (from-to)	281-286
Number of pages	6
Journal	Neuroscience Letters
Volume	44
Issue number	3
DOIs	https://doi.org/10.1016/0304-3940(84)90036-3
State	Published - Feb 24 1984

Keywords

amino-phosphono-heptanoic acid
excitatory receptors
kainic acid
l-glutamate
peptides

ASJC Scopus subject areas

General Neuroscience

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10.1016/0304-3940(84)90036-3

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title = "Glutamate-containing dipeptides enhance specific binding at glutamate receptors and inhibit specific binding at kainate receptors in rat brain",

abstract = "The dipeptide, l-phenylalanyl-l-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [3H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 μM with an EC50 of 4.9 μM. The increase in the specific binding of [3H]AHP induced by PG results exclusively from an increase in Bmax. In contrast, PG inhibits the specific binding of [3H]kainic acid to forebrain membranes with a Ki of 6.8 μM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [3H]APH and kainate receptors modulated by glutamate-containing peptides.",

keywords = "amino-phosphono-heptanoic acid, excitatory receptors, kainic acid, l-glutamate, peptides",

author = "J. Ferkany and R. Zaczek and A. Markl and Coyle, {J. T.}",

note = "Funding Information: This research was supported by USPHS Grants NS 13584, NS 18414, Fellowship NS 06798 and RSDA Type II MH00125. We thank Dorothea K. Stieff for her excellent technical assistance. Copyright: Copyright 2014 Elsevier B.V., All rights reserved.",

year = "1984",

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doi = "10.1016/0304-3940(84)90036-3",

language = "English (US)",

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pages = "281--286",

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AU - Ferkany, J.

AU - Zaczek, R.

AU - Markl, A.

AU - Coyle, J. T.

N1 - Funding Information: This research was supported by USPHS Grants NS 13584, NS 18414, Fellowship NS 06798 and RSDA Type II MH00125. We thank Dorothea K. Stieff for her excellent technical assistance. Copyright: Copyright 2014 Elsevier B.V., All rights reserved.

PY - 1984/2/24

Y1 - 1984/2/24

N2 - The dipeptide, l-phenylalanyl-l-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [3H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 μM with an EC50 of 4.9 μM. The increase in the specific binding of [3H]AHP induced by PG results exclusively from an increase in Bmax. In contrast, PG inhibits the specific binding of [3H]kainic acid to forebrain membranes with a Ki of 6.8 μM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [3H]APH and kainate receptors modulated by glutamate-containing peptides.

AB - The dipeptide, l-phenylalanyl-l-glutamate (PG), augments the specific binding of the excitatory amino acid receptor antagonist, [3H]2-amino-7-phosphonoheptanoic acid (APH), to rat forebrain membranes by 5-fold at 100 μM with an EC50 of 4.9 μM. The increase in the specific binding of [3H]AHP induced by PG results exclusively from an increase in Bmax. In contrast, PG inhibits the specific binding of [3H]kainic acid to forebrain membranes with a Ki of 6.8 μM. Of several related peptides examined, active ones affected the two receptor sites in a reciprocal fashion. The results suggest an allosteric interaction between [3H]APH and kainate receptors modulated by glutamate-containing peptides.

KW - amino-phosphono-heptanoic acid

KW - excitatory receptors

KW - kainic acid

KW - l-glutamate

KW - peptides

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ER -

Glutamate-containing dipeptides enhance specific binding at glutamate receptors and inhibit specific binding at kainate receptors in rat brain

Abstract

Keywords

ASJC Scopus subject areas

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