Clark C R, Gee S J, Krieger R I
Pharmacology. 1978;17(4):201-9. doi: 10.1159/000136855.
Pretreatment of 3 male rhesus monkeys (Macaca mulatta) with SKF 525-A(20 mg/kg, i.m.) 3 h prior to to injecting 14CH3-N-antipyrine (30 mg/kg, i.v.) increased antipyrine plasma half-life (APH) 240--500%; measurements of APH made 4, 8 and 11 days after SKF 525-A treatment were also higher than control values. Increases correspond to decreased plasma levels of 3-hydroxymethylantipyrine and 4-hydroxyantipyrine and decreased rates of aldrin epoxidation in liver biopsy homogenates. Comparison of HSLC and radiometric methods for determining APH showed that both methods were capable of detecting chemically altered hepatic monooxygenase activity.
在给3只雄性恒河猴(猕猴)静脉注射14C甲基安替比林(30毫克/千克)前3小时,肌肉注射SKF 525 - A(20毫克/千克)进行预处理,可使安替比林血浆半衰期(APH)延长240% - 500%;在SKF 525 - A治疗后第4、8和11天测得的APH也高于对照值。这种增加与血浆中3 - 羟甲基安替比林和4 - 羟基安替比林水平降低以及肝活检匀浆中艾氏剂环氧化速率降低相对应。比较用于测定APH的高效液相色谱法和放射性测量法表明,这两种方法都能够检测到化学改变的肝单加氧酶活性。