2. Academic Validation
  3. Vasorelaxant activity of phthalazinones and related compounds

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.
Esther del Olmo 1,  Bianca Barboza,  Maria Inés Ybarra,  José Luis López-Pérez,  Rosalía Carrón,  Maria Angeles Sevilla,  Cinthia Boselli,  Arturo San Feliciano
Affiliations

Affiliation

  • 1 Departamento de Química Farmacéutica, CISET, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain. olmo@usal.es
PMID: 16513345 DOI: 10.1016/j.bmcl.2006.02.003
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.

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