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Molecular Pharmacology

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Abstract

Effects of bromowillardiine and willardiine on non-N-methyl-D-aspartate receptors in postnatal rat hippocampal neurons.

C F Zorumski, L L Thio and D B Clifford
Molecular Pharmacology July 1991, 40 (1) 45-51;
C F Zorumski
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L L Thio
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D B Clifford
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Abstract

The physiology and pharmacology of willardiine and bromowillardiine, structural analogues of quisqualate, were studied in cultured postnatal rat hippocampal neurons using whole-cell voltage-clamp techniques. These agonists appear to act at a shared non-N-methyl-D-aspartate (non-NMDA) receptor-channel complex and gate nonselective cationic currents. Willardiine currents desensitize rapidly and to a much greater degree than bromowillardiine currents. In addition, the brominated compound produces steady state currents that are 5 times larger than those produced by willardiine at saturation. Bromowillardiine is also a more efficacious excitotoxin, producing about 3-fold greater acute neuronal damage than willardiine at saturating concentrations. These results suggest that agonist structure affects the ability of non-NMDA agonists to induce desensitization and add support to the hypothesis that receptor desensitization serves to limit acute excitotoxicity in cultured neurons.

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Molecular Pharmacology
Vol. 40, Issue 1
1 Jul 1991
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Abstract

Effects of bromowillardiine and willardiine on non-N-methyl-D-aspartate receptors in postnatal rat hippocampal neurons.

C F Zorumski, L L Thio and D B Clifford
Molecular Pharmacology July 1, 1991, 40 (1) 45-51;

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Abstract

Effects of bromowillardiine and willardiine on non-N-methyl-D-aspartate receptors in postnatal rat hippocampal neurons.

C F Zorumski, L L Thio and D B Clifford
Molecular Pharmacology July 1, 1991, 40 (1) 45-51;
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