Zin'kovskiĭ V G, Golovenko N Ia, Bogatskiĭ A V
Biull Eksp Biol Med. 1981;91(1):40-2.
A method has been suggested for simultaneous recording of the content of 12C-phenazepam and its metabolites in the mouse brain and of minimum effective doses of corasole intravenously that induce the tonic extension of the animals. Parameters of the two-compartmental kinetic model of absorption, distribution and elimination of 14C-products in the mouse brain were determined. These processes conform to the first order kinetics. A correlation was disclosed between the content of radioactive products in the animals' brain and minimum effective doses of corasole. A linear decline of the anticonvulsant action of phenazepam was revealed during the experimental period. Radiochromatography enabled one to detect the parent compound and its 3-hydroxy metabolite in mouse brain extracts.
已提出一种方法,用于同时记录小鼠脑中12C-芬那西泮及其代谢物的含量以及静脉注射诱导动物强直性伸展的最小有效剂量的可拉佐。确定了小鼠脑中14C产物吸收、分布和消除的二室动力学模型参数。这些过程符合一级动力学。揭示了动物脑中放射性产物含量与可拉佐最小有效剂量之间的相关性。在实验期间发现芬那西泮的抗惊厥作用呈线性下降。放射色谱法能够检测小鼠脑提取物中的母体化合物及其3-羟基代谢物。