Guanidine derivative U-37883A, inhibits mitochondrial K+ uniport

Pol J Pharmacol. 1995 Jul-Aug;47(4):339-44.

Abstract

The activity of potassium uniport in rat liver mitochondria was measured using light scattering technique (mitochondrial swelling). It was shown, that guanidine derivative, U-37883A (4-morpholinecarboxamidine-N-1-adamantyl-N'-cyclohexylhyd rochloride), was able to inhibit A23187 induced potassium uniport activity. The inhibitory effect of U-37883A on mitochondrial swelling gave an IC50 an of 89 +/- microM. No inhibition was observed with U-37883A analog, U-42069D (4-morpholinecarboxamidine), which points to the specificity of U-37883A action. It was also shown, that U-37883A acted on a different binding site in rat liver mitochondria than glibenclamide, inhibitor of the ATP sensitive potassium channel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adamantane / analogs & derivatives*
  • Adamantane / pharmacology
  • Animals
  • Binding, Competitive
  • Diuretics / pharmacology*
  • Dose-Response Relationship, Drug
  • Mitochondria / drug effects*
  • Morpholines / pharmacology*
  • Potassium / metabolism*
  • Potassium Channels / drug effects*
  • Rats

Substances

  • Diuretics
  • Morpholines
  • Potassium Channels
  • U 37883A
  • Adamantane
  • Potassium