ラジオレセプターアッセイによる中枢神経作用薬の徴量定量法の確立とラットにおける体内動態解析への応用

概要

論文の詳細を見る
Simple and sensitive methods are developed for microdetermination of drugs acting on the central nervous system. The assay employs the partially purified synaptosomal membrane isolated from rat brain. In the assay, 3H-Quinuclidinyl benzylate competes with drugs for binding to the receptor. The detection limit for scopolamine was 20 ng/ml. This method was applied for the measurement of other drugs acting on the central nervous system. The values of IC 50 were lower than 0.1μg/ml in biperiden, trihexyphenidyl, levomepromazine, and promethazine. The method has been used to determine plasma levels in 9-week-old and 21-week-old rats after i.v. injection of 1 mg/kg scopolamine. The blood levels of scopolamine at each time after the administration are significantly different between 9-week-old and 21-week-old rats. The values of V_<dss> determined in 21-week-old rats were significantly increased as compared to the 9-week-old rats, whereas CL_<tot> were not changed.
日本医療薬学会の論文
1993-03-20