左旋和右旋吡喹酮在人和大鼠肝微粒体内的代谢  

Metabolism of (-)- and (+)-praziquantel in human andrat liver microsomes

作　　者：何坎 全钰珠[1] 

机构地区：[1]重庆医科大学药理教研室

出　　处：《中国药理学与毒理学杂志》1993年第3期210-213,共4页Chinese Journal of Pharmacology and Toxicology

摘　　要：左旋吡喹酮[(-)PQT]在人和大鼠肝微粒体中人谢生成产物[M];在[M]色谱峰处,右旋吡喹酮[(+)PQT]无明显代谢物生成.人肝微粒体代谢(?)-PQT生成MI的K_m和V_(max)分别为58±s13μmol·L^1和1.3±s 0.6 nmol·mg^1·min^1·RF.在人肝微粒体中,(?)与(+)PQT原药消除的K_m和V_(max)比值分别为0.86±s 0.28和1.5±s 0.5;(-)-和(+)PQT人肝内在清除率分别为1.3±s 0.5和0.7±s0.3 ml·h^1·mg^1,(-)-/(+)PQT的比值平均为1.8±s 0.5(-)与(-)-PQT在大鼠肝微粒体中消除速率的比值为1.83±s 0.27。Both human and rat livermicrosomes formed one metabolite from(-)-praziquantel(PQT)with the same retention time as M I formed in rabbit liver microsomes,and in the case of(+)-PQT,however,no clear M I absorption peak was found on the chromatogram for both liver microsomes.The Cli of(-)-and(+)-PQT by human liver microsomes was 1.3±s 0.5 and 0.7±s 0.3 ml·h-1·.mg-1 protein,respectively.The former was significantly higher than the latter with an average ratio of 1.8±s 0.5.As measured by parent drug disappearance,(-)-/(+)-PQT ratio of Vmax and of Km was 1.5±s 0.5 and 0.86±s 0.28 respectively.Km and Kmax measured by M I formation from(-)-PQT were 58±s 13μmol·L-1 and 1.3±s 0.6 nmol·mg-1·min-1·response factor,respectively.Rat liver microsomes also preferentially metabolize(-)-PQT and the ratio of(-)-to(+)-PQT disappearance rate was 1.83±s 0.27.

关 键 词：吡喹酮 对映异构体 代谢 肝微粒体 

分 类 号：R965[医药卫生—药理学]