二苯乙内酰脲底物诱导的差异光谱：其他抗惊厥药物的抑制作用

Diphenylhydantoin substrate induced difference spectra: inhibition by other anticonvulsant drugs.

作者信息

Patsalos P N, Lascelles P T

出版信息

Res Commun Chem Pathol Pharmacol. 1980 Jan;27(1):31-43.

Abstract

The ability of five commonly used anticonvulsants to produce substrate induced difference specta was assessed. Only diphenylhydantoin (DPH) and phenobarbitone were observed to produce such spectra and were of Type I. Mean Ks values for DPH and phenobarbitone were 6.8 x 10(-5) and 4.0 x 10(-4)M, respectively. The anticonvulsants sulthiame, ethosuximide, sodium valproate and phenobarbitone exhibited inhibition of DPH substrate induced difference spectra to varying degrees. Analysis of data as in the classical enzyme/inhibitor models resulted in mean Ksi values for the four anticonvulsants of 1.3 x 10(-4), 0.53 x 10(-2), 3.0 x 10(-3), and 6.8 x 10(-3), respectively. Inhibition of DPH substrate induced difference spectra by sulthiame and phenobarbitone was strong and competitive. Inhibition by ethosuximide was weak and competitive, while sodium valproate's inhibition was weak and uncompetitive.

摘要

评估了五种常用抗惊厥药产生底物诱导差异光谱的能力。仅观察到苯妥英（DPH）和苯巴比妥能产生此类光谱，且属于I型。DPH和苯巴比妥的平均Ks值分别为6.8×10⁻⁵和4.0×10⁻⁴M。抗惊厥药舒噻美、乙琥胺、丙戊酸钠和苯巴比妥对DPH底物诱导的差异光谱有不同程度的抑制作用。按照经典酶/抑制剂模型对数据进行分析，这四种抗惊厥药的平均Ksi值分别为1.3×10⁻⁴、0.53×10⁻²、3.0×10⁻³和6.8×10⁻³。舒噻美和苯巴比妥对DPH底物诱导的差异光谱的抑制作用较强且具有竞争性。乙琥胺的抑制作用较弱且具有竞争性，而丙戊酸钠的抑制作用较弱且为非竞争性。