Biphenyl酢酸誘導体の蛋白結合

概要

論文の詳細を見る
Protein binding of 4'-chloro-5-methoxy-3-biphenylylacetic acid (DKA-9), a newly developed anti-inflammatory agent, and its metabolites was examined using the equilibrium dialysis method. It was found from Scatchard plot data that they were bound strongly to bovine serum albumin and had two or more binding sites on the albumin molecule. The binding parameters were as follows : K_1=2×10^4 M^<-1>, K_2=8×10^2 M^<-1>, n_1=11.5,n_2=27.1 and these values were comparable with K_1 of salicylic acid and quinidine, and of K_1×n_1 of phenylbutazone. In order to obtain a clue to the understanding of the species differences in ADME studies, the binding behavior of DKA-9 to various animal plasma was also investigated. The binding parameters were obtained from the modified Scatchard plot analysis and it was found that there were considerable species differences. It was also suggested that there was a correlation between the species difference in protein binding and that in drug elimination rate.
公益社団法人日本薬学会の論文
1978-03-25