3-Alkyl- and 3-aryl-7H-furo[3,2-g]chromen-7-ones as blockers of the voltage-gated potassium channel Kv1.3

Pharmazie. 2004 Apr;59(4):319-20.

Abstract

3-Alkyl- and 3-aryl-7H-furo[3,2-g]chromen-7-ones were synthesised and studied for their effects on voltage-gated K+ and Na+ channels of the neuroblastoma cell-line N1E-115 and K+ channels of L-929 mouse-fibroblasts, stably transfected with mKv1.3. All furocoumarins tested showed Kv channel blocking activities, the most potent one in a half-blocking concentration of 0.7 microM.

MeSH terms

  • Animals
  • Brain Neoplasms / metabolism
  • Cell Line, Tumor
  • Cells, Cultured
  • Coumarins / chemical synthesis*
  • Coumarins / pharmacology*
  • Fibroblasts
  • Humans
  • Ion Channel Gating / drug effects
  • Kv1.3 Potassium Channel
  • Membrane Potentials / drug effects
  • Mice
  • Neuroblastoma / metabolism
  • Patch-Clamp Techniques
  • Potassium Channel Blockers / chemical synthesis*
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channels / drug effects*
  • Potassium Channels, Voltage-Gated*
  • Sodium Channel Blockers / chemical synthesis
  • Sodium Channel Blockers / pharmacology

Substances

  • Coumarins
  • KCNA3 protein, human
  • Kcna3 protein, mouse
  • Kv1.3 Potassium Channel
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Voltage-Gated
  • Sodium Channel Blockers