Boobis A R, Murray S, Hampden C E, Davies D S
Biochem Pharmacol. 1985 Jan 1;34(1):65-71. doi: 10.1016/0006-2952(85)90101-7.
A sensitive, specific assay utilizing fluorescence-HPLC has been developed for determining the 1'-hydroxylation of bufuralol by human liver. The 1'-hydroxylation of the isomers of bufuralol varied threefold, both the Vmax and the Km for the (+) isomer being greater than the corresponding values for the (-) isomer. Debrisoquine was a competitive inhibitor of the 1'-hydroxylation of both isomers and of the racemate of bufuralol. Both isomers and the racemate of bufuralol were competitive inhibitors of debrisoquine 4-hydroxylase activity. The competitive inhibition of debrisoquine and bufuralol of each other's metabolism, together with the similarity in the values for Km and Ki, support the conclusion that the same form of cytochrome P-450 catalyses these two reactions.
已开发出一种利用荧光高效液相色谱法的灵敏、特异的检测方法，用于测定人肝脏对布呋洛尔的1'-羟化作用。布呋洛尔异构体的1'-羟化作用变化了三倍，(+)异构体的Vmax和Km均大于(-)异构体的相应值。去甲异喹胍是两种异构体以及布呋洛尔外消旋体1'-羟化作用的竞争性抑制剂。布呋洛尔的两种异构体和外消旋体都是去甲异喹胍4-羟化酶活性的竞争性抑制剂。去甲异喹胍和布呋洛尔对彼此代谢的竞争性抑制作用，以及Km和Ki值的相似性，支持了同一形式的细胞色素P-450催化这两种反应的结论。
