Inhibition of the 5-HT3 receptor-mediated current by the protein kinase inhibitor, H-7

Brain Res. 1994 Jun 27;649(1-2):310-2. doi: 10.1016/0006-8993(94)91078-2.

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

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

Substances

  • Ion Channels
  • Isoquinolines
  • Piperazines
  • Protein Kinase Inhibitors
  • Receptors, Serotonin
  • Serotonin
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine