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5-苯甲酰基-α-甲基-2-噻吩乙酸(噻洛芬酸)对过敏性豚鼠心脏类花生酸释放的调节作用

Modulation of eicosanoid release from anaphylactic guinea-pig heart with 5-benzoyl-a-methyl-2-thiophene acetic acid (tiaprofenic acid).

作者信息

Simmet T, Wittenberg H R, Peskar B A

出版信息

Arch Int Pharmacodyn Ther. 1985 Dec;278(2):207-14.

PMID:3841634
Abstract

The effects of infusion of the non-steroidal anti-inflammatory drugs (NSAID), tiaprofenic acid (2.2 micrograms/min or 10.0 micrograms/min) and indomethacin (1.0 microgram/min) on the release of leukotriene (LT) C4-like immunoreactivity, thromboxane (TX) B2 and 6-keto-prostaglandin (PG) F1 alpha from isolated perfused anaphylactic guinea-pig hearts were investigated. Tiaprofenic acid at both concentrations used significantly inhibited anaphylactic release of TXB2 and 6-keto-PGF1 alpha as did indomethacin (1.0 microgram/min) which was, however, about ten times more potent in this respect. Release of immunoreactive LTC4-like material was not influenced by the lower concentration of tiaprofenic acid used (2.2 micrograms/min), but significantly enhanced by the higher concentration (10.0 micrograms/min). Thus, the effect of tiaprofenic acid on eicosanoid release by the anaphylactic heart is very similar to that of indomethacin without any differential inhibition of TXB2 or 6-keto-PGF1 alpha formation.

摘要

研究了输注非甾体抗炎药(NSAID)替洛芬酸(2.2微克/分钟或10.0微克/分钟)和吲哚美辛(1.0微克/分钟)对离体灌注的过敏豚鼠心脏中白三烯(LT)C4样免疫反应性、血栓素(TX)B2和6-酮-前列腺素(PG)F1α释放的影响。所用的两种浓度的替洛芬酸均显著抑制TXB2和6-酮-PGF1α的过敏释放,吲哚美辛(1.0微克/分钟)也有此作用,不过在这方面其效力约强十倍。较低浓度(2.2微克/分钟)的替洛芬酸对免疫反应性LTC4样物质的释放没有影响,但较高浓度(10.0微克/分钟)则使其显著增强。因此,替洛芬酸对过敏心脏类花生酸释放的作用与吲哚美辛非常相似,对TXB2或6-酮-PGF1α的形成没有任何差异抑制作用。

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