Inhibitory effects of ethaverine, a homologue of papaverine, on dopamine content in PC12 cells

Biol Pharm Bull. 2001 Jan;24(1):103-5. doi: 10.1248/bpb.24.103.

Abstract

The inhibitory effects of ethaverine on dopamine content in PC12 cells were investigated. Ethaverine decreased dopamine content in a concentration-dependent manner in PC12 cells and showed 33.6% inhibition of dopamine content at a concentration of 1.0 microM for 24-48 h. The IC50 value of ethaverine was 1.4 microM. Dopamine content was lowered at 6h and reached a minimal level at 12h after exposure to ethaverine at 2.0 microM. The decreased dopamine level was maintained up to 48 h and then recovered to the control level at about 72 h. Tyrosine hydroxylase (TH) was inhibited at 6 h following treatment with ethaverine in PC12 cells and the activity was maintained at a reduced level up to 36 h (12-22% inhibition at 2.0 microM). These results indicate that ethaverine leads to a decrease in dopamine content by inhibition of TH activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, L-Type / drug effects
  • Dopamine / biosynthesis
  • Dopamine / metabolism*
  • Enzyme Inhibitors / pharmacology
  • PC12 Cells
  • Papaverine / analogs & derivatives*
  • Papaverine / pharmacology*
  • Rats
  • Tyrosine 3-Monooxygenase / antagonists & inhibitors

Substances

  • Calcium Channel Blockers
  • Calcium Channels, L-Type
  • Enzyme Inhibitors
  • ethaverine
  • Papaverine
  • Tyrosine 3-Monooxygenase
  • Dopamine