Tsuboi T, Hatano N, Nakatsuji K, Fujitani B, Yoshida K, Shimizu M, Kawasaki A, Sakata M, Tsuboshima M
Arch Int Pharmacodyn Ther. 1980 Sep;247(1):89-102.
Effects of OP 1206 were studied on the cardiovascular system and platelet functions to assess OP 1206 as an antianginal agent. OP 1206 given orally at more than 100 micrograms/kg relieved vasopressin-induced ST depression of rat electrocardiogram (ECG), an animal model of angina pectoris, concomitant with slight hypotension. Intra-coronary injection of OP 1206 (1-100 ng/kg) in dogs resulted in a remarkable increase of coronary blood flow without any influence on heart rate, blood pressure, myocardial oxygen consumption and redox potential. Resistance in both large and small vessels of dog coronary artery was decreased by intravenous injection of OP 1206 (1-3 micrograms/kg). Platelet aggregation, adhesiveness, bleeding time, and thrombocytopenia induced by ADP and collagen infusion in guinea-pigs were inhibited by oral administration of OP 1206 at the same doses or doses less than those relieving vasopressin-induced ST depression of ECG. These results suggest that OP 1206 contributes to the improvement of cardiac imbalance between oxygen demand and supply, and suppression of thrombus formation in atherosclerotic heart.
研究了OP 1206对心血管系统和血小板功能的影响,以评估OP 1206作为抗心绞痛药物的作用。以超过100微克/千克的剂量口服OP 1206可减轻血管加压素诱导的大鼠心电图(ECG)ST段压低,这是一种心绞痛动物模型,同时伴有轻微低血压。在犬冠状动脉内注射OP 1206(1-100纳克/千克)可显著增加冠状动脉血流量,而对心率、血压、心肌耗氧量和氧化还原电位无任何影响。静脉注射OP 1206(1-3微克/千克)可降低犬冠状动脉大、小血管的阻力。以相同剂量或低于减轻血管加压素诱导的ECG ST段压低的剂量口服OP 1206可抑制豚鼠因输注ADP和胶原蛋白引起的血小板聚集、黏附性、出血时间和血小板减少。这些结果表明,OP 1206有助于改善心脏氧供需失衡,并抑制动脉粥样硬化性心脏病中的血栓形成。