@article {Zorumski45, author = {C F Zorumski and L L Thio and D B Clifford}, title = {Effects of bromowillardiine and willardiine on non-N-methyl-D-aspartate receptors in postnatal rat hippocampal neurons.}, volume = {40}, number = {1}, pages = {45--51}, year = {1991}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, 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.}, issn = {0026-895X}, URL = {https://molpharm.aspetjournals.org/content/40/1/45}, eprint = {https://molpharm.aspetjournals.org/content/40/1/45.full.pdf}, journal = {Molecular Pharmacology} }