Fan L L, Sun L H, Lin Y
Department of Pharmacology, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1997 Nov;32(11):808-12.
The cardiotonic and vasodilating effects of oxyphenamone were studied in preparations of rat Langendorff's heart, isolated cardiac muscles of guinea pigs and isolated arteries of dogs. In the preparations of rat Langendorff's heart, infusion of oxyphenamone at 0.1 and 1.0 mumol.L-1 increased myocardial contractility and coronary blood flow moderately and decreased heart rate slightly. Oxyphenamone (1-100 mumol.L-1) increased the contractile force of papillary muscle (PM) and left atrium (LA) of guinea pigs dose-dependently. The positive inotropic effect of oxyphenamone (the ED50 was found to be 18.35 mumol.L-1 in PM and 9.17 mumol.L-1 in LA) was close to that of milrinone, an inhibitor of phosphodiesterase(the ED50 was shown to be 6.23 mumol.L-1 in PM and 4.59 mumol.L-1 in LA). The difference between these two agents is that oxyphenamone decreased the spontaneous pulse rate of right atrium, while milrinone increased it. The vasoconstrictions of dog coronary, basilar and mesenteric arteries induced by KCl, 5-HT and CaCl2 were antagonized non-competitively by oxyphenamone at 1 and 50 mumol.L-1, suggesting that oxyphenamone has a relaxant effect on vascular smooth muscles.
在大鼠Langendorff心脏标本、豚鼠离体心肌和犬离体动脉中研究了奥昔苯酮的强心和血管舒张作用。在大鼠Langendorff心脏标本中，以0.1和1.0μmol·L-1的浓度输注奥昔苯酮可适度增加心肌收缩力和冠状动脉血流量，并轻微降低心率。奥昔苯酮（1-100μmol·L-1）剂量依赖性地增加豚鼠乳头肌（PM）和左心房（LA）的收缩力。奥昔苯酮的正性肌力作用（PM中的ED50为18.35μmol·L-1，LA中的ED50为9.17μmol·L-1）与磷酸二酯酶抑制剂米力农相近（PM中的ED50为6.23μmol·L-1，LA中的ED50为4.59μmol·L-1）。这两种药物的不同之处在于，奥昔苯酮降低右心房的自发搏动率，而米力农则增加该速率。1和50μmol·L-1的奥昔苯酮对氯化钾、5-羟色胺和氯化钙诱导的犬冠状动脉、基底动脉和肠系膜动脉的血管收缩有非竞争性拮抗作用，提示奥昔苯酮对血管平滑肌有舒张作用。
