Kawashima K, Kuzuya T, Matsuda A
Diabetes. 1979 Mar;28(3):221-6. doi: 10.2337/diab.28.3.221.
A specific, sensitive, and simple radioimmunoassay was developed for the oral hypoglycemic drug glibenclamide, N-4-[2-(5-chloro-2-methoxy-benzamide)-ethyl]-benzenesulfonyl-N'-cyclohexylurea. Antiserum against glibenclamide was obtained from rabbits immunized with an antigen prepared by conjugating the diazonium salt of N(p-amino-benzamidoethyl)-benzenesulfonyl-N'-cyclohexylurea to bovine serum albumin through the diazocoupling. [3H]glibenclamide was used as a tracer. Dextran-coated charcoal was used to separate bound and free [3H]glibenclamide in the reaction mixture. The radioimmunoassay is able to determine as little as 25 pg of glibenclamide directly in plasma without the need for extraction. The antiserum used for the assay was highly specific for glibenclamide, and did not cross-react with two known major metabolites of glibenclamide. Comparable values of glibenclamide in dog plasma were obtained by radioimmunoassay and liquid chromatography. Plasma concentrations of glibenclamide in diabetic patients on glibenclamide treatment can be determined by radioimmunoassay, and the method has been applied to the routine assay of clinical samples. This radioimmunoassay seems to be useful for monitoring plasma glibenclamide concentrations.
已开发出一种针对口服降糖药格列本脲（N-4-[2-(5-氯-2-甲氧基-苯甲酰胺)-乙基]-苯磺酰基-N'-环己基脲）的特异性强、灵敏度高且操作简便的放射免疫分析法。用通过重氮偶联将N-(对氨基苯甲酰胺基乙基)-苯磺酰基-N'-环己基脲的重氮盐与牛血清白蛋白偶联制备的抗原免疫家兔，获得了抗格列本脲的抗血清。[3H]格列本脲用作示踪剂。葡聚糖包被的活性炭用于分离反应混合物中结合型和游离型的[3H]格列本脲。该放射免疫分析法能够直接测定血浆中低至25 pg的格列本脲，无需萃取。用于该分析的抗血清对格列本脲具有高度特异性，且不与格列本脲的两种已知主要代谢产物发生交叉反应。通过放射免疫分析法和液相色谱法获得的犬血浆中格列本脲的值具有可比性。接受格列本脲治疗的糖尿病患者血浆中格列本脲的浓度可通过放射免疫分析法测定，该方法已应用于临床样本的常规检测。这种放射免疫分析法似乎对监测血浆格列本脲浓度很有用。
