咖啡因作为一种代谢探针：用于评估CYP1A2活性的代谢比的比较。
Caffeine as a metabolic probe: a comparison of the metabolic ratios used to assess CYP1A2 activity.
作者信息
Notarianni L J, Oliver S E, Dobrocky P, Bennett P N, Silverman B W
机构信息
School of Pharmacy and Pharmacology, University of Bath.
出版信息
Br J Clin Pharmacol. 1995 Jan;39(1):65-9. doi: 10.1111/j.1365-2125.1995.tb04411.x.
Abstract
- Caffeine is widely used as an in vivo probe for CYP1A2; the distribution/activity of this enzyme is reported to be reflected by metabolic ratios. 2. Several metabolic ratios using different combinations of urinary metabolites have been used to measure CYP1A2, with varying conclusions on its distribution. 3. A mathematical comparison of five metabolic ratios claiming to reflect CYP1A2 activity was made using data from 237 healthy volunteers. 4. All five metabolic ratios were symmetrically distributed. The five ratios however, measured at least three different parameters, with no one ratio correlating exactly with any other. 5. Data in the literature claiming to measure CYP1A2 using caffeine may reflect other parameters. 6. The complex metabolism of caffeine together with different parameters controlling the renal clearance of each metabolite, makes the use of urinary metabolic ratios an inaccurate probe for assessing the distribution of CYP1A2 activity in populations.
摘要
- 咖啡因被广泛用作细胞色素P450 1A2（CYP1A2）的体内探针；据报道，该酶的分布/活性可通过代谢率反映出来。2. 几种使用不同尿代谢物组合的代谢率已被用于测定CYP1A2，但其分布情况结论不一。3. 利用237名健康志愿者的数据，对声称能反映CYP1A2活性的五种代谢率进行了数学比较。4. 所有五种代谢率均呈对称分布。然而，这五种代谢率至少测量了三个不同的参数，且没有一种代谢率与其他任何一种完全相关。5. 文献中声称使用咖啡因测定CYP1A2的数据可能反映了其他参数。6. 咖啡因复杂的代谢过程以及控制每种代谢物肾脏清除率的不同参数，使得使用尿代谢率作为评估人群中CYP1A2活性分布的探针并不准确。
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Genetic control of isoniazid metabolism in man.人体中异烟肼代谢的遗传控制。
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Accelerated caffeine metabolism after omeprazole treatment is indicated by urinary metabolite ratios: coincidence with plasma clearance and breath test.尿代谢物比率表明奥美拉唑治疗后咖啡因代谢加速：与血浆清除率及呼气试验结果相符。
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Caffeine as a probe for CYP1A2 activity: potential influence of renal factors on urinary phenotypic trait measurements.咖啡因作为CYP1A2活性的探针：肾脏因素对尿表型特征测量的潜在影响。
Pharmacogenetics. 1994 Jun;4(3):117-24.
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