苯二氮䓬类药物放射受体分析法在毒理学中的应用。

Application of radioreceptor assay of benzodiazepines for toxicology.

作者信息

Aaltonen L, Scheinin M

出版信息

Acta Pharmacol Toxicol (Copenh). 1982 Mar;50(3):206-12. doi: 10.1111/j.1600-0773.1982.tb00963.x.

DOI:10.1111/j.1600-0773.1982.tb00963.x

Abstract

A radioreceptor assay (RRA) for determining benzodiazepines (BZ) has been developed and applied to toxicological analysis of serum from 21 patients with acute BZ overdosage. The method was sensitive (e.g., lorazepam 17 nM, diazepam 41 nM), and specific for pharmacologically active BZ derivatives. The reproducibility of the results was good (intra-assay variation less than 8%, inter-assay variation less than 10%). Concentrations measured by the RRA showed a good correlation with those obtained by gas-liquid chromatographic analysis of the same samples. The quantitative results represent the sum of one or several parent substances and all biologically active metabolites, in proportion to their receptor binding affinities.

摘要

已开发出一种用于测定苯二氮䓬类药物（BZ）的放射受体分析法（RRA），并将其应用于21例急性BZ过量患者血清的毒理学分析。该方法灵敏（例如，劳拉西泮为17 nM，地西泮为41 nM），且对具有药理活性的BZ衍生物具有特异性。结果的重现性良好（批内变异小于8%，批间变异小于10%）。通过RRA测定的浓度与对相同样品进行气液色谱分析所获得的浓度具有良好的相关性。定量结果代表一种或几种母体物质与所有生物活性代谢物之和，与其受体结合亲和力成比例。