Abstract
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.
MeSH terms
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1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
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Animals
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In Vitro Techniques
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Ion Channels / drug effects*
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Isoquinolines / pharmacology*
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Membrane Potentials / drug effects
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Nodose Ganglion / cytology
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Nodose Ganglion / drug effects
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Nodose Ganglion / metabolism
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Patch-Clamp Techniques
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Piperazines / pharmacology*
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Protein Kinase Inhibitors*
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Rats
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism*
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Serotonin / physiology*
Substances
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Ion Channels
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Isoquinolines
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Piperazines
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Protein Kinase Inhibitors
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Receptors, Serotonin
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Serotonin
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1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine