[阿西美辛药效学研究(作者译名)]。

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雅可比H，戴尔HD

[阿西美辛药效学研究(作者译名)]。

Arzneimittelforschung。1980;30(8):1348 - 62。

PubMed ID

6968219 (PubMed视图

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摘要

对新型强效非甾体抗炎药(1-(对氯苯甲酰)-5-甲氧基-2-甲基吲哚-3-乙酰氧基)乙酸(乙酰美辛，TV 1322，兰都地尔)进行药效学研究，阐明其作用机制。尽管阿西美辛具有很强的抗炎活性，但它只是一种弱的前列腺素释放抑制剂。乙酰美辛能明显抑制n -甲基同氨基苯胺甲醛缩合物(化合物48/80)诱导肥大细胞释放组胺，并呈剂量依赖性。它在体外试验中也非常有效，例如在水岛的蛋白质浊度试验中。由于该抗炎药对前列腺素释放的抑制作用较弱，对胃肠道粘膜的损伤很小。从这些数据和强抗炎活性可以得出广泛的治疗边际。镇痛作用表现在苯醌口服后的试验和im应用后的Randall-Selitto试验。吡铁和酵母引起的热疗被阿西美辛抑制，并呈剂量依赖性。与对前列腺素释放的微弱影响相对应的是，阿西美辛对利尿的抑制作用很小。体外实验未检测到妊娠子宫的抗宫缩作用。 Function of the heart (isolated heart of guinea-pig) was unaffected, but we registered an increase in sytolic and diastolic blood pressures in the anesthetized dog. Correspondingly, left ventricular pressure also increased, these changes were accompanied by bradycardia. Coronary flow, peripheral flow and dp/dt did not change, only the pressure in the right atrium rose slightly. In cats, acemetacin caused a short-lasting decrease in the arterial blood pressure. Effects on CNS were not found. Smooth muscles (bronchial/intestinal) were not influenced by acemetacin. Like many non-steroidal anti-inflammatory compounds acemetacin inhibits also platelet aggregation. Motility of animals was lowered. In a granuloma pouch test a strong anti-inflammatory action was shown in vivo even without metabolic degradation of acemetacin. For the explanation of the anti-inflammatory action several mechanisms have to be taken into account.

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药物

Acemetacin