1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）类似物对人苄胺氧化酶（BzAO）的抑制作用
Inhibition of human benzylamine oxidase (BzAO) by analogues of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP).
作者信息
Devlin A J, Bhatti A R, Williams A C, Ramsden D B
机构信息
Department of Medicine, University of Birmingham, Queen Elizabeth Hospital, Edgbaston, U.K.
出版信息
Toxicol Lett. 1990 Dec;54(2-3):135-42. doi: 10.1016/0378-4274(90)90176-m.
A sensitive assay for human plasma BzAO, involving the conversion of 14C-benzylamine to 14C-benzaldehyde, was developed. MPTP and several of its analogues were found to be competitive inhibitors of the enzyme. Ki values for the MPTP analogues in the presence of human plasma BzAO were determined. The analogues had a different rank order of inhibition of human plasma BzAO compared with the rank order of inhibition of bovine plasma BzAO found previously. MPTP and 1-methyl-4-(2-methylphenyl)-1,2,3,6-tetrahydropyridine (2'-CH3-MPTP), which are potent nigrostriatal toxins, were weak inhibitors of human plasma BzAO.
开发了一种用于检测人血浆中BzAO的灵敏检测方法，该方法涉及将14C-苄胺转化为14C-苯甲醛。发现MPTP及其几种类似物是该酶的竞争性抑制剂。测定了人血浆BzAO存在下MPTP类似物的Ki值。与先前发现的牛血浆BzAO的抑制顺序相比，这些类似物对人血浆BzAO的抑制顺序不同。MPTP和1-甲基-4-(2-甲基苯基)-1,2,3,6-四氢吡啶(2'-CH3-MPTP)是强效黑质纹状体毒素，它们是人血浆BzAO的弱抑制剂。
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