Vasorelaxant activity of phthalazinones and related compounds

Bioorg Med Chem Lett. 2006 May 15;16(10):2786-90. doi: 10.1016/j.bmcl.2006.02.003. Epub 2006 Mar 2.

Abstract

Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10(-5)M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC(50)=0.43microM) the affinities for alpha(1A), alpha(1B) and alpha(1D) adrenergic sub-receptors were determined.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Male
  • Phthalazines / chemistry
  • Phthalazines / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, Adrenergic, alpha / classification
  • Receptors, Adrenergic, alpha / drug effects
  • Vas Deferens / drug effects
  • Vas Deferens / physiology
  • Vasodilation / drug effects*

Substances

  • Phthalazines
  • Receptors, Adrenergic, alpha