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非甾体抗炎药对血小板聚集和血管张力的作用与抑制前列环素(PGI2)和血栓素释放的关系。特别提及5-苯甲酰基-α-甲基-2-噻吩乙酸(噻洛芬酸)。

The action of non-steroidal antiinflammatory agents on platelet aggregation and vessel tone in relation to inhibition of PGI2- and thromboxane-release. With particular reference to 5-benzoyl-alpha-methyl-2-thiophene acetic acid (tiaprofenic acid).

作者信息

Kuhn A, Sauerland S, Schiffer K, Schrör K

出版信息

Arzneimittelforschung. 1980;30(9):1538-42.

PMID:7006618
Abstract

The actions of 5-benzoyl-alpha-methyl-2-thiophene acetic acid (tiaprofenic acid) on platelet aggregation, coronary vascular tone and myocardial oxygen consumption were studied in vitro and compared to those of diclofenac sodium, indometacin and meclofenamate. Tiaprofenic acid dose-dependently and reversibly inhibited collagen- and arachidonic acid-induced aggregation of rabbit platelet-rich plasma (IC50 2--5 micromol/l) and was as effective in this system as the reference compounds. Tiaprofenic acid did not alter the myocardial oxygen consumption up to 120 micromol/l but produced reversible and dose-dependent increases in the coronary vascular tone of both guinea pig hearts and isolated bovine coronary arteries at 0.1--10 micromol/l concentrations. This coronary vasomotor activity of tiaprofenic acid could be correlated to its ability to inhibit the vascular PGI2 production whereas the inhibition of platelet aggregation by all of the substances studied does not seem to be tightly correlated to their inhibitory effect on the thromboxane formation of blood platelets.

摘要

研究了5-苯甲酰基-α-甲基-2-噻吩乙酸(噻洛芬酸)对血小板聚集、冠状血管张力和心肌耗氧量的作用,并在体外将其与双氯芬酸钠、吲哚美辛和甲氯芬那酸进行了比较。噻洛芬酸剂量依赖性且可逆地抑制胶原和花生四烯酸诱导的富含兔血小板血浆的聚集(IC50为2 - 5微摩尔/升),在该系统中与参比化合物效果相当。在浓度达120微摩尔/升时,噻洛芬酸不改变心肌耗氧量,但在0.1 - 10微摩尔/升浓度下,可使豚鼠心脏和离体牛冠状动脉的冠状血管张力产生可逆的剂量依赖性增加。噻洛芬酸的这种冠状血管舒缩活性可能与其抑制血管前列环素生成的能力相关,而所研究的所有物质对血小板聚集的抑制作用似乎与其对血小板血栓素形成的抑制作用没有紧密关联。

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