Activation of protein kinase C by phorbol dibutyrate potentiates [3H]MK-801 binding in rat brain slices.
Effects of activation of protein kinase C (PKC) on N-methyl-D-aspartate) NMDA receptor function were analyzed by quantitative autoradiography using [3H]MK-801 in rat brain slices. The density of [3H]MK-801 binding was highest in hippocampus and high levels were found in cortex, striatum and thalamus. Levels in brainstem and molecular layer of cerebellum were low. The receptor binding was markedly decreased in almost all areas by addition of 2. 5 mM Mg2+. After activation of PKC by 100 nM phorbol-12, 13-dibutyrate (PDBu), [3H]MK-801 binding was increased in most areas, but binding levels were not changed in brainstem and cerebellum. The elevated [3H]MK-801 binding produced by PDBu was significantly inhibited by addition of Mg2+ except in inferior colliculus and cerebellum. These results suggest that activation of PKC potentiates NMDA receptor function in a region-specific manner in the rat brain.
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Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson, MS 39216-4045, USA.
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D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology* / Q000502:physiology; D001923:Brain Chemistry / Q000187:drug effects / Q000502:physiology; D016291:Dizocilpine Maleate / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D066298:In Vitro Techniques; D015240:Phorbol 12,13-Dibutyrate / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D011493:Protein Kinase C / Q000378:metabolism*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism / Q000502:physiology
D016194:Receptors, N-Methyl-D-Aspartate; D015240:Phorbol 12,13-Dibutyrate; D016291:Dizocilpine Maleate; D011493:Protein Kinase C