Creveling C R, Kirk K L
Biochem Biophys Res Commun. 1985 Aug 15;130(3):1123-31. doi: 10.1016/0006-291x(85)91732-2.
The three ring-fluorinated analogs of dihydroxyphenylalanine (DOPA) were synthesized and the kinetics of their O-methylation catalyzed by catechol-O-methyltransferase compared to those of DOPA. The affinities (Km) of 2-FDOPA, 5-FDOPA, DOPA, and 6-FDOPA were 20, 23, 55, and 552 microM, respectively, whilst the Vmax values were 4.0, 4.4, 5.0 and 5.4 nmol per min per mg protein. The importance of the low affinity and decreased rate constant of 6-FDOPA for COMT are discussed with regard to the use of 6-FDOPA as an 18-fluorine labeled probe for positron emission transaxial tomography (PETT).
合成了二羟基苯丙氨酸（DOPA）的三种环氟化类似物，并将其由儿茶酚-O-甲基转移酶催化的O-甲基化动力学与DOPA的进行了比较。2-氟-DOPA、5-氟-DOPA、DOPA和6-氟-DOPA的亲和力（Km）分别为20、23、55和552微摩尔，而Vmax值分别为每分钟每毫克蛋白质4.0、4.4、5.0和5.4纳摩尔。关于将6-氟-DOPA用作正电子发射断层扫描（PETT）的18氟标记探针，讨论了6-氟-DOPA对儿茶酚-O-甲基转移酶的低亲和力和降低的速率常数的重要性。
