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Piperofurol(MD 710247)是一种苯并呋喃的衍生物。小剂量静脉给药可增加麻醉狗的冠脉流量和冠脉窦血氧分压,并可减慢心率和降低血压。曾假设本品可能是一种钙拮抗药,本文报道的离体实验数据支持此论点。研究表明,在离体狗冠状动脉的近侧段及远侧段,本品可抑制高钾去极化所致的收缩,此作用与剂量相关。其半数抑制浓度(IC_(50))分别为20nM和27nM,此作用较其他钙拮抗药为强(如戊脉安为320nM和100nM)。增高营养液中Ca~(++)浓度可去除piperofurol的抑制作用。在兔胸主动脉的pA_2值为9.1。在离体豚鼠乳头肌,本品(1.1μM)使动作电位时程延长(+50%),最大上升速率减慢(-52%),并使收缩力减弱,此作用与浓度有关(0.2～1.1μM)。在存在
Piperofurol (MD 710247) is a benzofuran derivative. Small doses of intravenous administration can increase the coronary flow of anesthetized dogs and coronary sinus partial pressure of oxygen, and can slow down the heart rate and lower blood pressure. It has been assumed that this product may be a calcium antagonist, the in vitro data reported in this article supports this argument. Studies have shown that in isolated proximal and distal coronary arteries, this product can inhibit high potassium depolarization induced contraction, the role of dose-related. The median inhibitory concentration (IC 50) was 20 nM and 27 nM, respectively, which was stronger than other calcium antagonists (eg, verapamil 320 nM and 100 nM). Increasing the concentration of Ca ~ (++) in nutrient solution can remove the inhibitory effect of piperofurol. The pA_2 value in rabbit thoracic aorta was 9.1. In vitro guinea pig papillary muscles, the goods (1.1μM) action potential duration (+ 50%), the maximum rate of slowdown (-52%), and to reduce contractility, the role of concentration (0.2 ~ 1.1 μM). In existence