Kinetic analysis of interactions between kainate and AMPA: evidence for activation of a single receptor in mouse hippocampal neurons.
AMPA but not kainate produces a rapidly desensitizing response in mouse hippocampal neurons. The characteristic action of these agonists appears to arise from activation of a single receptor with active and desensitized states, for which AMPA and kainate have different relative affinity. The equilibrium potency of a series of five agonists that produce rapidly desensitizing responses at non-NMDA receptors (EC50 1 microM to 4 mM) was similar to their equilibrium potency for block of kainate responses. Increasing the concentration of kainate overcame such block, but in the presence of AMPA the rate of activation of responses to kainate was slowed. Conversely, in the presence of kainate the amplitude of rapidly desensitizing responses evoked by AMPA was reduced, and the rate of onset of desensitization was slowed.
Patneau
D K
DK
Laboratory of Developmental Neurobiology, National Institutes of Health, Bethesda, Maryland 20892.
Mayer
M L
ML
D000818:Animals; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004336:Drug Antagonism; D004594:Electrophysiology; D005971:Glutamates / Q000494:pharmacology; D018698:Glutamic Acid; D006624:Hippocampus / Q000187:drug effects / Q000196:embryology* / Q000502:physiology; D007051:Ibotenic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D007608:Kainic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D051379:Mice; D009474:Neurons / Q000187:drug effects* / Q000502:physiology; D016318:Quisqualic Acid / Q000494:pharmacology; D018092:Kainic Acid Receptors; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
D005971:Glutamates; D018698:Glutamic Acid; D007051:Ibotenic Acid; D007608:Kainic Acid; D016318:Quisqualic Acid; D018092:Kainic Acid Receptors; D017981:Receptors, Neurotransmitter; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; C012301:domoic acid