A new class of powerful inhibitors of monamine oxidase A.
A new class of powerful inhibitors of monamine oxidase A.
复制标题
一类新型强效单胺氧化酶 A 抑制剂。
DOI：
10.1016/0006-291x(90)91596-k
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发表时间：
1990
影响因子：
3.1
通讯作者：
Singer,TP
中科院分区：
文献类型：
--
作者：
Jin,YZ;Ramsay,RR;Youngster,SK;Singer,TP
1-甲基-4-苯基-1，2，3，6-四氢吡啶（MPTP）的神经毒性生物活化产物1-甲基-4-苯基吡啶鎓（MPP）及其大多数类似物是单胺氧化酶A的良好竞争性抑制剂，Ki值在微摩尔范围内，但它们仅在高得多的浓度下抑制单胺氧化酶B。本文报道了在芳环4′位取代的MPP+的烷基衍生物是A型酶的更有效的可逆抑制剂，Ki值在纳摩尔范围内（0.075 - 1.6 μM）。仅在高出2 - 3个数量级的浓度（32-374 μM）下才能抑制B型酶。
It is well established that 1-methyl-4-phenylpyridinium (MPP), the neurotoxic bioactivation product of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and most of its analogs are good competitive inhibitors of monoamine oxidase A, with Kivalues in the micromolar range, but they inhibit monoamine oxidase B only at much higher concentrations. We report here the finding that alkyl derivatives of MPP+substituted at the 4′ position of the aromatic ring are considerably more effective reversible inhibitors of the A type enzyme, with Kivalues in the nanomolar range (0.075 –1.6 μM). They inhibit the B type enzyme only at 2 to 3 orders of magnitude higher concentrations (32–374 μM).