Evaluation of the Biological Activity of Several Analogs of the Dopaminergic Neurotoxin 1‐Methyl‐4‐Phenyl‐1,2,3,6‐Tetrahydropyridine
Evaluation of the Biological Activity of Several Analogs of the Dopaminergic Neurotoxin 1‐Methyl‐4‐Phenyl‐1,2,3,6‐Tetrahydropyridine
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多巴胺能神经毒素 1-甲基-4-苯基-1,2,3,6-四氢吡啶的几种类似物的生物活性评价
DOI：
10.1111/j.1471-4159.1987.tb05606.x
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发表时间：
1987
影响因子：
4.7
通讯作者：
R. Heikkila
中科院分区：
文献类型：
--
作者：
S. Youngster;Patricia K. Somalia;R. Heikkila
Abstract: Several analogs of l‐methyl‐4‐phenyl‐l,2,3,6‐tetrahydropyridine (MPTP) were synthesized and screened for their capacity to be oxidized by monoamine oxidase (MAO‐A or MAO‐B) and their capacity to produce nigrostriatal dopaminergic neurotoxicity in mice. All of the compounds were relatively weak substrates for MAO‐A but many of the compounds were found to be good substrates for MAO‐B. Only three of the compounds, in addition to MPTP itself, were found to be neurotoxic. These were 1‐methyl‐4‐cyclohexyl‐1,2,3,6‐tetrahydropyridine, 1 ‐methyl‐4‐(2′‐methylphenyl)‐1,2,3,6‐tetrahydropyridine and 1‐methyl‐4‐(3′‐methoxyphenyl)‐1,2,3,6‐tetrahydropyridine. All three of these neurotoxic compounds were found to be substrates for MAO‐B; in contrast no compound was found to be neurotoxic that was not oxidized by MAO‐B. The capacity of the compounds studied to be oxidized by MAO‐B appears to be an important aspect of the neurotoxic process.
影响因子：
6.1
作者：
CASTAGNOLI, N;CHIBA, K;TREVOR, AJ
通讯作者：
TREVOR, AJ
DOI：
10.1073/pnas.82.7.2173
发表时间：
1985-01-01
影响因子：
11.1
作者：
JAVITCH, JA;DAMATO, RJ;SNYDER, SH
通讯作者：
SNYDER, SH