title: Vasorelaxant activity of phthalazinones and related compounds.
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.
authors.affiliation: Departamento de Química Farmacéutica, CISET, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain. olmo@usal.es
authors.forename: Esther
authors.initials: E
authors.lastname: del Olmo
authors.forename: Bianca
authors.initials: B
authors.lastname: Barboza
authors.forename: Maria Inés
authors.initials: MI
authors.lastname: Ybarra
authors.forename: José Luis
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Rosalía
authors.initials: R
authors.lastname: Carrón
authors.forename: Maria Angeles
authors.initials: MA
authors.lastname: Sevilla
authors.forename: Cinthia
authors.initials: C
authors.lastname: Boselli
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
mesh_terms: D000818:Animals; D008297:Male; D010793:Phthalazines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011942:Receptors, Adrenergic, alpha / Q000145:classification / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects / Q000502:physiology; D014664:Vasodilation / Q000187:drug effects*
chemical_list: D010793:Phthalazines; D011942:Receptors, Adrenergic, alpha