Drsata J, Pribová M, Hais I M
Cesk Farm. 1989 Nov;38(9):407-10.
The effect of the novel Czechoslovak antiphlogistic agent flobufen (VUFB 16066, 4-[2',4'-difluorbiphenyl]-4-oxo-methyl-butanic acid) and its metabolite 2',4'-difluorbiphenyl-4-yl acetic acid (VUFB 17203) on decarboxylase of aromatic amino acids (DAAK, E. C. 4.1.1.28) of the rat liver (supernatant 20,000 x g) was studied in vitro. The concentrations of 3.8 x 10(-4) mol x 1(-1) of flobufen and 4.4 x 10(-4) mol x 1(-1) of difluorbiphenylyl acetic acid produced 50% inhibition n the enzyme. Ki for flobufen is approximately 1.5 x 10(-4) mol x 1(-1), the reaction with the inhibitor takes place in the ratio 1:1 and the enzyme-inhibitor complex does not exert any catalytic activity. In the tissues with a low activity of DAAK, inhibition could be manifested by decreased synthesis of serotonin and dopamine.
研究了新型捷克斯洛伐克抗炎药氟比洛芬（VUFB 16066，4-[2',4'-二氟联苯]-4-氧代-甲基-丁酸）及其代谢产物2',4'-二氟联苯-4-基乙酸（VUFB 17203）对大鼠肝脏（20,000 x g上清液）芳香族氨基酸脱羧酶（DAAK，E.C. 4.1.1.28）的体外作用。氟比洛芬浓度为3.8 x 10(-4) mol x 1(-1) 以及二氟联苯乙酸浓度为4.4 x 10(-4) mol x 1(-1) 时对该酶产生50% 的抑制作用。氟比洛芬的抑制常数（Ki）约为1.5 x 10(-4) mol x 1(-1)，与抑制剂的反应按1:1进行，且酶-抑制剂复合物不发挥任何催化活性。在DAAK活性较低的组织中，抑制作用可能表现为血清素和多巴胺合成减少。
