Inhibition of the 5-HT3 receptor-mediated current by the protein kinase inhibitor, H-7.
The effect of the protein kinase inhibitor, H-7, on the inward current mediated by 5-HT3 receptors was investigated with the whole-cell patch-clamp technique. H-7 inhibited the peak 5-HT current with an IC50 of 1.79 microM. The inhibition was quick, reversible and not blocked by the presence of 50 microM intracellular H-7. It is concluded that the effect of H-7 was independent of protein kinase activity.
Fan
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Laboratory of Molecular and Cellular Neurobiology, National Institute on Alcohol Abuse and Alcoholism, Rockville, MD 20852.
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D000818:Animals; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects*; D007546:Isoquinolines / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D009620:Nodose Ganglion / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D018408:Patch-Clamp Techniques; D010879:Piperazines / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012701:Serotonin / Q000502:physiology*
D007473:Ion Channels; D007546:Isoquinolines; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011985:Receptors, Serotonin; D012701:Serotonin; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine