一种碱性抗炎剂盐酸2-氨甲基-4-叔丁基-6-碘苯酚（MK-447）对前列腺素内过氧化物生物合成的双重作用。

Dual effects of a basic anti-inflammatory agent, 2-aminomethyl-4-t-butyl-6-iodophenol hydrochloride (MK-447), on biosynthesis of prostaglandin endoperoxides.

作者信息

Harada Y, Tanaka K, Katori M

出版信息

Jpn J Pharmacol. 1980 Aug;30(4):549-57. doi: 10.1254/jjp.30.549.

DOI:10.1254/jjp.30.549

Abstract

Effects of MK-447 on prostaglandin (PG) endoperoxide formation from arachidonic acid by bovine seminal vesicle microsomes in the presence of cofactors (hemoglobin and tryptophan) were studied by cascade superfusion on rabbit aorta and mesenteric artery and rat stomach and colon. In the presence of hemoglobin (0.2 muM), MK-447 (up to 30 muM) accelerated PG endoperoxide formation, as tryptophan did, whereas higher concentrations of MK-447 lost the acceleration effect and finally inhibited the PG endoperoxide formation. Increased concentration of hemoglobin (2 muM) shifted the dose of MK-447 for peak generation from 30 to 100 muM. Thus, MK-447 shows dual action, acceleration and inhibition, on the PG endoperoxide formation.

摘要

通过对兔主动脉和肠系膜动脉以及大鼠胃和结肠进行级联灌注，研究了MK - 447在辅因子（血红蛋白和色氨酸）存在下对牛精囊微粒体从花生四烯酸形成前列腺素（PG）内过氧化物的影响。在血红蛋白（0.2 μM）存在的情况下，MK - 447（高达30 μM）像色氨酸一样加速PG内过氧化物的形成，而更高浓度的MK - 447则失去加速作用并最终抑制PG内过氧化物的形成。血红蛋白浓度增加（2 μM）使MK - 447产生峰值的剂量从30 μM变为100 μM。因此，MK - 447对PG内过氧化物的形成表现出加速和抑制的双重作用。

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Dual effects of a basic anti-inflammatory agent, 2-aminomethyl-4-t-butyl-6-iodophenol hydrochloride (MK-447), on biosynthesis of prostaglandin endoperoxides.一种碱性抗炎剂盐酸2-氨甲基-4-叔丁基-6-碘苯酚（MK-447）对前列腺素内过氧化物生物合成的双重作用。

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