Stygles V G, Commassaris R A, Rech R H, Hook J B
Arch Int Pharmacodyn Ther. 1978 Sep;235(1):43-50.
The ability of indoprofen or sodium indoprofen to inhibit phenylquinone-writhing and renal prostaglandin synthesis was determined in mice following a single oral dose of either drug. Male mice (4/group) were treated with 1.5 mg/kg indoprofen or sodium indoprofen. Inhibition of phenylquinone-writhing was determined at 2, 4, 8, 16 and 32 hr post treatment. Animals were sacrificed and blood collected for determination of plasma indoprofen concentration. Kidneys were removed and prepared for determination of renal prostaglandin synthesis by an in vitro technique. Phenylquinone-writhing was significantly depressed by both preparations at 2 and 4 hr post treatment. Sodium indoprofen also significantly depressed writhing at 8 hr post treatment. Renal prostaglandin synthesis, like phenylquinone-writhing, was significantly depressed at 2 and 4 hr after drug treatment. Plasma indoprofen concentration was correlated with both inhibition of phenylquinone-wrighing and inhibition of renal prostaglandin synthesis. When writhes were plotted versus prostaglandin synthesis, a positive correlation was observed suggesting a temporal relationship between inhibition of phenylquinone-writhing and inhibition of renal prostaglandin synthesis.
单次口服吲哚美辛或吲哚美辛钠后,在小鼠中测定了它们抑制苯醌扭体反应和肾脏前列腺素合成的能力。雄性小鼠(每组4只)接受1.5mg/kg吲哚美辛或吲哚美辛钠治疗。在治疗后2、4、8、16和32小时测定对苯醌扭体反应的抑制作用。处死动物并采集血液以测定血浆吲哚美辛浓度。取出肾脏并通过体外技术制备用于测定肾脏前列腺素合成的样本。两种制剂在治疗后2和4小时均显著抑制苯醌扭体反应。吲哚美辛钠在治疗后8小时也显著抑制扭体反应。与苯醌扭体反应一样,药物治疗后2和4小时肾脏前列腺素合成显著受到抑制。血浆吲哚美辛浓度与苯醌扭体反应的抑制和肾脏前列腺素合成的抑制均相关。当将扭体次数与前列腺素合成作图时,观察到正相关,表明苯醌扭体反应的抑制与肾脏前列腺素合成的抑制之间存在时间关系。