RO-4-4602对儿茶酚-O-甲基转移酶的竞争性抑制作用。
Competitive inhibition of catechol O-methyltransferase by RO-4-4602.
作者信息
Buu N T, Kuchel O, Parent M T
出版信息
Can J Biochem. 1977 Jul;55(7):771-3. doi: 10.1139/o77-112.
RO-4-4602, a peripheral L-DOPA decarboxylase (EC 4.1.1.28) inhibitor was shown to also inhibit the activity of catechol O-methyltransferase (COMT) (EC 2.1.1.6). Kinetic study indicated that the inhibition is of a competitive nature. The apparent Ki values of 7 X 10(6), 5.3 X 10(-6, and 9 X 10-6) M calculated from Lineweaver-Burke plots when dopamine, norepinephrine, and epinephrine, respectively, were used as substrate, showed that this drug is the most potent inhibitor of COMT yet known.
RO-4-4602，一种外周L-多巴脱羧酶（EC 4.1.1.28）抑制剂，已被证明还能抑制儿茶酚-O-甲基转移酶（COMT）（EC 2.1.1.6）的活性。动力学研究表明，这种抑制作用具有竞争性。当分别以多巴胺、去甲肾上腺素和肾上腺素作为底物，根据Lineweaver-Burke图计算得出的表观Ki值分别为7×10⁻⁶、5.3×10⁻⁶和9×10⁻⁶ M，这表明该药物是目前已知的最有效的COMT抑制剂。
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