Vasorelaxing properties of some phenylacridine type potassium channel openers in isolated rabbit thoracic arteries

Eur J Med Chem. 2002 Jun;37(6):519-23. doi: 10.1016/s0223-5234(02)01374-0.

Abstract

In this study, 12 new 2,2,7,7-tetramethyl-9-aryl-2,3,4,5,6,7,9,10-octahydro-1,8-acridindione derivatives were synthesised and their effects on vascular potassium channels and mechanism of induced relaxations on phenylephrine-induced contractile responses in isolated rabbit thoracic arteries was investigated. Pinacidil was used as standard potassium channel openers in this study. Compounds 1-12 and pinacidil exerted concentration-dependent relaxation responses precontracted phenylephrine in the aortic rings with the efficacy order: 11>pinacidil>7>2>8>3>1>4>10>6>9>5>12.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / pharmacology*
  • Animals
  • Aorta, Thoracic / drug effects
  • Glyburide / pharmacology
  • Hypoglycemic Agents / pharmacology
  • In Vitro Techniques
  • Kinetics
  • Magnetic Resonance Spectroscopy
  • Male
  • Molecular Weight
  • Muscle, Smooth, Vascular / drug effects*
  • Phenylephrine / antagonists & inhibitors
  • Pinacidil / pharmacology
  • Potassium Channels / agonists*
  • Rabbits
  • Tetraethylammonium Compounds / pharmacology
  • Vasoconstrictor Agents / antagonists & inhibitors
  • Vasodilator Agents / chemical synthesis*
  • Vasodilator Agents / pharmacology*

Substances

  • Acridines
  • Hypoglycemic Agents
  • Potassium Channels
  • Tetraethylammonium Compounds
  • Vasoconstrictor Agents
  • Vasodilator Agents
  • Phenylephrine
  • Pinacidil
  • Glyburide