Waldmeier P C, De Herdt P, Maitre L
Research Department, Ciba-Geigy Ltd., Basel, Switzerland.
J Neural Transm Suppl. 1990;32:381-6. doi: 10.1007/978-3-7091-9113-2_52.
Methods potentially suitable for the determination of the COMT inhibitory properties of CGP 28014 (N-(2-pyridone-6-yl)-N',N'-di-n-propylformamidine) in humans were tested in rats: the measurement of effects on HVA levels and on the conversion of exogenously administered L-DOPA into its O-methylated derivative, in serum and striatum. The compound decreased HVA as well as the conversion of L-DOPA to O-methyl-DOPA similarly in serum and striatum. The latter parameter was considered to be more useful for the assessment of COMT inhibition in humans, because it is less affected by diurnal changes, dietary effects, physical activity etc.
在大鼠中测试了可能适用于测定人CGP 28014（N-（2-吡啶酮-6-基）-N'，N'-二正丙基甲脒）的儿茶酚-O-甲基转移酶（COMT）抑制特性的方法：测量其对高香草酸（HVA）水平以及对外源性给予的左旋多巴（L-DOPA）在血清和纹状体中转化为其O-甲基化衍生物的影响。该化合物在血清和纹状体中同样降低了HVA以及L-DOPA向O-甲基多巴（O-methyl-DOPA）的转化。后一个参数被认为对评估人类的COMT抑制更有用，因为它受昼夜变化、饮食影响、身体活动等的影响较小。
