Skolnick P, Goodwin F K, Paul S M
Arch Gen Psychiatry. 1979 Jan;36(1):78-80. doi: 10.1001/archpsyc.1979.01780010084009.
We describe a rapid and sensitive radioreceptor assay for measuring benzodiazepines in plasma. This method is based on the competition between tritiated diazepam and pharmacologically active benzodiazepines present in plasma, for binding sites on rat brain synaptosomal membranes. No interference is obtained with drug-free plasma or plasma samples containing high concentrations of other commonly used drugs. High correlations (r = 0.98; P less than .001) were obtained between the "diazepam equivalents" measured in plasma with the radioreceptor assay and the levels of diazepam and nordiazepam obtained by gas-liquid chromatography. The radioreceptor assay is rapid, sensitive, specific, and requires no sophisticated equipment or methods. It should therefore prove useful in monitoring blood benzodiazepine levels for both therapeutic and toxicologic purposes.
我们描述了一种用于测量血浆中苯二氮䓬类药物的快速灵敏的放射受体测定法。该方法基于氚标记地西泮与血浆中存在的药理活性苯二氮䓬类药物竞争大鼠脑突触体膜上的结合位点。不含药物的血浆或含有高浓度其他常用药物的血浆样本均无干扰。通过放射受体测定法测得的血浆中“地西泮等效物”与通过气液色谱法测得的地西泮和去甲地西泮水平之间具有高度相关性(r = 0.98;P小于0.001)。放射受体测定法快速、灵敏、特异,且不需要复杂的设备或方法。因此,它在治疗和毒理学目的监测血液苯二氮䓬类药物水平方面应会证明是有用的。