Radioimmunoassay for the synthetic ergoline derivative cabergoline in biological fluids.
Radioimmunoassay for the synthetic ergoline derivative cabergoline in biological fluids.
复制标题
生物体液中合成麦角林衍生物卡麦角林的放射免疫测定。
DOI：
10.1080/15321819208021243
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发表时间：
1992
期刊：
影响因子：
--
通讯作者：
M. S. Benedetti
中科院分区：
文献类型：
--
作者：
S. Persiani;E. Pianezzola;F. Broutin;G. Fonte;M. S. Benedetti
卡麦角林是一种有效的多巴胺激动剂，正在进行临床试验，用于治疗帕金森氏病和高催乳素血症。通过将卡麦角林与牛血清白蛋白偶联产生的免疫原免疫兔子，制备了卡麦角林的抗血清。该抗血清能够与氚标记的卡麦角林衍生物结合，并能够将药物分子与其一些密切相关的化合物以及接受卡麦角林治疗的患者的血浆中同时存在的其他药物区分开来。用抗血清和氚标记的半抗原建立了测定人血、尿中卡麦角林的放射免疫分析方法。卡麦角林的加入量与放射性结合百分率在1.9-500pg/管范围内呈线性关系。加入200微升人血浆或25微升尿液不影响放射性标记半抗原的特异性和非特异性结合，从而使我们能够获得大约12pg/ml血浆和120pg/ml尿液的最终灵敏度。在血浆和尿液中检测的整个浓度范围内，该分析的重复性、精密度和准确度都得到了验证。用该方法测定了一例帕金森病患者每日单次口服3、5和7 mg后的稳态血药浓度。
An antiserum against cabergoline, a powerful dopamine-agonist under clinical trials for the treatment of Parkinson's disease and hyperprolactinemia, has been raised in rabbits by immunization with an immunogen produced by conjugation of cabergoline to bovine serum albumin. The antiserum was able to bind a derivative of cabergoline labelled with tritium and was able to distinguish the drug molecule from some of its close related compounds and from other agents that could be simultaneously present in plasma from patients undergoing treatment with cabergoline. The antiserum and the tritium labelled hapten were used to develop a radioimmunoassay for cabergoline determination in human plasma and urine. A linear relationship between cabergoline added and % radioactivity bound was found in the range 1.9-500 pg/tube. The addition in the assay of 200 microliters human plasma or 25 microliters urine did not affect the specific and the non-specific binding of the radiolabelled hapten so enabling us to obtain a final sensitivity of about 12 pg/ml plasma and 120 pg/ml urine. The assay was validated in terms of reproducibility, precision and accuracy over the whole range of concentrations tested both in plasma and urine. The plasma concentrations at the steady state in a patient with Parkinson's disease who had received the drug at single oral daily doses of 3, 5 and 7 mg were determined using the assay.