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人体内抗变应原剂2-甲氧基-11-氧代-11-H-吡啶并[2,1-b]喹唑啉-8-羧酸的放射免疫测定及血浆浓度

Radioimmunoassay and plasma concentrations of the anti-allergenic agent, 2-methoxy-11-oxo-11-H-pyrido[2,1-b]quinazoline-8-carboxylic acid in man.

作者信息

Dixon R, Lucek R, Liu Y Y, Colburn W, Parsonnet M

出版信息

Res Commun Chem Pathol Pharmacol. 1980 Oct;30(1):163-70.

PMID:7433765
Abstract

A specific radioimmunoassay (RIA) for the determination of the antiallergenic agent, 2-methoxy-11-oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acid (I), directly in plasma has been developed employing a rabbit antiserum to an albumin conjugate of I. The RIA has a limit of sensitivity of 0.4 ng/ml of I using a 0.1 ml sample of plasma. The intra- and interassay coefficients of variation did not exceed 6 and 9%, respectively. The specificity of the RIA was established by comparison with a less sensitive high-performance liquid chromatographic procedure and excellent agreement (r = 0.98) was observed when plasma samples were assayed by both methods. The RIA was used to determine plasma concentrations of I in man, for the first time, following oral administration of single 2, 10 and 50 mg doses of the drug.

摘要

已开发出一种特异性放射免疫分析法(RIA),用于直接测定血浆中的抗变应原剂2-甲氧基-11-氧代-11H-吡啶并[2,1-b]喹唑啉-8-羧酸(I),该方法采用针对I的白蛋白结合物的兔抗血清。使用0.1 ml血浆样品时,该放射免疫分析法对I的检测限为0.4 ng/ml。批内和批间变异系数分别不超过6%和9%。通过与灵敏度较低的高效液相色谱法进行比较,确定了该放射免疫分析法的特异性,当用两种方法检测血浆样品时,观察到两者具有极好的一致性(r = 0.98)。首次使用该放射免疫分析法测定了人单次口服2、10和50 mg剂量该药物后血浆中I的浓度。

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