Protein kinase inhibitor, H-7, directly affects N-methyl-D-aspartate receptor channels.
Compounds commonly used to modify protein phosphorylation have been found to interact directly with K channels, Ca channels, and acetylcholine receptor channels. We report that a general protein kinase inhibitor, H-7, directly affects N-methyl-D-aspartate (NMDA) receptors independent of protein kinase activity. Single-channel records in the presence of H-7 have fewer bursts of activity, and the currents are interrupted in a voltage-dependent manner by brief closures. Hippocampal whole-cell currents induced by NMDA are not decreased by H-7, in part, because the single-channel currents have longer burst lengths that compensate for the brief closures.
Amador
M
M
Department of Molecular Physiology and Biophysics, Baylor College of Medicine, Houston, TX 77030.
Dani
J A
JA
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D000818:Animals; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000494:pharmacology*; D008274:Magnesium / Q000494:pharmacology; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D010879:Piperazines / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects*
D007546:Isoquinolines; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D016194:Receptors, N-Methyl-D-Aspartate; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D008274:Magnesium