Yuan A S, Hand E L, Hichens M, Olah T V, Barrish A, Fernandez-Metzler C, Gilbert J D
Merck Research Laboratories, West Point, PA 19486.
J Pharm Biomed Anal. 1993 Jun;11(6):427-34. doi: 10.1016/0731-7085(93)80153-r.
MK-852 is a novel fibrinogen receptor antagonist. A sensitive and specific radioimmunoassay has been developed for the determination of this drug candidate in plasma and urine. The immunogen was prepared by coupling to albumin via a dinitrophenylene bridge and the radioligand by reaction of the drug with the 125I-labelled Bolton-Hunter reagent. The method was specific and no immunoreactive material other than parent drug was detectable in plasma from dosed volunteers. The direct assay using 0.05 ml of plasma is sensitive to 0.2 ng ml-1 without matrix interference and has sufficient sensitivity, precision, accuracy, and selectivity for the analysis of clinical samples. The lower quantifiable limit in (diluted) urine is 50 ng ml-1.
MK-852是一种新型纤维蛋白原受体拮抗剂。已开发出一种灵敏且特异的放射免疫分析法,用于测定血浆和尿液中的这种候选药物。免疫原通过二硝基苯桥与白蛋白偶联制备,放射性配体则通过药物与125I标记的博尔顿-亨特试剂反应制备。该方法具有特异性,给药志愿者的血浆中除母体药物外未检测到其他免疫反应性物质。使用0.05 ml血浆的直接分析法对0.2 ng/ml敏感,无基质干扰,对临床样品分析具有足够的灵敏度、精密度、准确度和选择性。(稀释后)尿液中的最低可定量限为50 ng/ml。