Vasorelaxant activity of phthalazinones and related compounds.
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.
del Olmo
Esther
E
Departamento de Química Farmacéutica, CISET, Facultad de Farmacia, Universidad de Salamanca, 37007 Salamanca, Spain. olmo@usal.es
Barboza
Bianca
B
Ybarra
Maria Inés
MI
López-Pérez
José Luis
JL
Carrón
Rosalía
R
Sevilla
Maria Angeles
MA
Boselli
Cinthia
C
San Feliciano
Arturo
A
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*
D010793:Phthalazines; D011942:Receptors, Adrenergic, alpha