Budriesi R, Rampa A, Bisi A, Fabbri G, Chiarini A, Valenti P
Department of Pharmaceutical Sciences, University of Bologna, Italy.
Arzneimittelforschung. 1995 Mar;45(3):234-9.
A series of some benzazepinone derivatives were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. For the compounds bearing well-known alpha-blocking fragments, the antagonist potency at postsynaptic alpha-adrenoceptors was assessed. The new compounds were less effective as bradycardic agents and calcium antagonists but show remarkable negative inotropic activity.
制备了一系列苯并氮杂䓬酮衍生物。对这些化合物的变力性、变时性和钙拮抗特性进行了评估。对于带有知名α-阻断片段的化合物,评估了其对突触后α-肾上腺素能受体的拮抗效力。新化合物作为心动过缓剂和钙拮抗剂的效果较差,但显示出显著的负性变力活性。