用于治疗药物监测的血液中氯硝西泮和地西泮的放射受体测定法。

Radioreceptor assay of clonazepam and diazepam in blood for therapeutic drug monitoring.

作者信息

Nishikawa T, Nishida A, Ohtani H, Sunaoshi W, Miura H, Sudo Y, Kubo H

机构信息

School of Medicine, Kitasato University, Kanagawa, Japan.

出版信息

Ther Drug Monit. 1989;11(4):483-6.

PMID:2500757

Abstract

Rat cerebral cortex was used to prepare a suspension of benzodiazepine receptors. The suspension was mixed with an extract of specimen and [3H]flunitrazepam. The mixture was filtered through a membrane, and radioactivity on the membrane was measured. Clonazepam concentrations in patient plasma specimens determined by radioreceptor assay and gas-liquid chromatography agreed well. However, diazepam equivalent concentrations determined by radioreceptor assay were close to the sum of diazepam and desmethyldiazepam concentrations determined by high-performance liquid chromatography, as desmethyldiazepam had binding activity for the receptor. This receptor assay method is accurate, simple, requires less than 0.5 ml of plasma, and is therefore suitable for analyzing numerous samples in a short time.

摘要

用大鼠大脑皮层制备苯二氮䓬受体悬浮液。将该悬浮液与标本提取物和[³H]氟硝西泮混合。混合物通过膜过滤，并测量膜上的放射性。通过放射受体分析法和气相色谱法测定的患者血浆标本中氯硝西泮浓度结果吻合良好。然而，通过放射受体分析法测定的地西泮等效浓度接近于通过高效液相色谱法测定的地西泮和去甲地西泮浓度之和，因为去甲地西泮对该受体具有结合活性。这种受体分析方法准确、简单，所需血浆量少于0.5毫升，因此适合在短时间内分析大量样本。