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Molecular Pharmacology

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Abstract

Zinc is a mixed antagonist of homomeric rho 1 gamma-aminobutyric acid-activated channels.

Y Chang, J Amin and D S Weiss
Molecular Pharmacology March 1995, 47 (3) 595-602;
Y Chang
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J Amin
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D S Weiss
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Abstract

The transition metal Zn2+ is differentially distributed in the central nervous system, where it is proposed to be a neuromodulator. One of the documented effects of Zn2+ is the antagonism of gamma-aminobutyric acid (GABA)-mediated synaptic inhibition. This antagonism is presumed to result from a direct interaction of Zn2+ with the GABA receptor/ionophore complex, although the characteristics of Zn2+ sensitivity are dependent on the particular GABA subunit combination. In this study, we examined the effects of Zn2+ on homomeric rho 1 GABA-activated channels expressed in Xenopus oocytes. Zn2+ was found to be a mixed antagonist of these recombinant rho 1 GABA receptors. The antagonism was predominantly competitive at low Zn2+ concentrations (< or = 100 microM), whereas at high Zn2+ concentrations (> 100 microM) a noncompetitive antagonism was apparent. Evidence is presented showing that the antagonism was not due to an interaction of GABA and Zn2+ in solution but, rather, resulted from interactions of these two ligands with the GABA-activated channel. A mechanism is proposed for Zn(2+)-mediated antagonism in which GABA and Zn2+ bind to distinct sites on the GABA complex. The apparent mixed antagonism may arise from different Ki values for the binding of Zn2+ to non-agonist-bound or agonist-bound receptors. However, two distinct Zn2+ binding sites, one competitive and one noncompetitive, could also give rise to the dual antagonism.

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Molecular Pharmacology
Vol. 47, Issue 3
1 Mar 1995
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Abstract

Zinc is a mixed antagonist of homomeric rho 1 gamma-aminobutyric acid-activated channels.

Y Chang, J Amin and D S Weiss
Molecular Pharmacology March 1, 1995, 47 (3) 595-602;

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Abstract

Zinc is a mixed antagonist of homomeric rho 1 gamma-aminobutyric acid-activated channels.

Y Chang, J Amin and D S Weiss
Molecular Pharmacology March 1, 1995, 47 (3) 595-602;
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