西维因三室毒代动力学及抗胆碱酯酶活性

Carbaryl tricompartmental toxicokinetics and anticholinesterase activity.

作者信息

Fernandez Y, Falzon M, Cambon-Gros C, Mitjavila S

出版信息

Toxicol Lett. 1982 Oct;13(3-4):253-8.

Abstract

The blood kinetics of carbaryl and the inhibition of plasma acetylcholinesterases were followed for 24 h after administration of 20 mg/kg [14C]carbaryl (0.17 microCi/mg). The kinetics of the radioactivity attributed to unaltered carbaryl is bi-exponential whereas that of the total 14C activity is tri-exponential. The kinetics were treated with open 2- and 3-compartment models respectively. The exchange rate constants between the various compartments as well as the elimination constant (expressed in h-1) were found to be: k12 = 1.93, k21 = 1.18 and k10 = 2.46 (2-compartment model) and k'12 = 18.65, k'21 = 13.90, k'13 = 1.14 k'31 = 0.125 and k'10 = 0.672 (3-compartment model). The 3-compartment model demonstrates the persistence in the blood of 14C activity which correlated with plasma acetylcholinesterase inhibition.

摘要

给予20mg/kg[¹⁴C]西维因（0.17微居里/毫克）后，跟踪观察西维因的血液动力学以及血浆乙酰胆碱酯酶的抑制情况，持续24小时。归因于未改变的西维因的放射性动力学呈双指数型，而总¹⁴C活性的动力学呈三指数型。分别用开放的二室和三室模型处理动力学。发现各室之间的交换速率常数以及消除常数（以h⁻¹表示）为：k12 = 1.93，k21 = 1.18，k10 = 2.46（二室模型）以及k'12 = 18.65，k'21 = 13.90，k'13 = 1.14，k'31 = 0.125，k'10 = 0.672（三室模型）。三室模型显示¹⁴C活性在血液中的持续存在，这与血浆乙酰胆碱酯酶抑制相关。