PT  - JOURNAL ARTICLE
AU  - Zorumski, C F
AU  - Thio, L L
AU  - Clifford, D B
TI  - Effects of bromowillardiine and willardiine on non-N-methyl-D-aspartate receptors in postnatal rat hippocampal neurons.
DP  - 1991 Jul 01
TA  - Molecular Pharmacology
PG  - 45--51
VI  - 40
IP  - 1
4099  - http://molpharm.aspetjournals.org/content/40/1/45.short
4100  - http://molpharm.aspetjournals.org/content/40/1/45.full
SO  - Mol Pharmacol1991 Jul 01; 40
AB  - 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.