Effect of various decarboxylase inhibitors on the cerebral metabolism of dihydroxyphenylalanine
Effect of various decarboxylase inhibitors on the cerebral metabolism of dihydroxyphenylalanine
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各种脱羧酶抑制剂对二羟基苯丙氨酸脑代谢的影响
DOI：
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发表时间：
1969
期刊：
影响因子：
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通讯作者：
A. Pletscher
中科院分区：
文献类型：
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作者：
G. Bartholini;A. Pletscher
小剂量脱羧酶(DC)抑制剂Ro 44602[N-(~~-seryl)-N’-(2，3，4-trihydroxybenzyl)hydrazine]，可增强多巴所致大鼠脑内儿茶酚胺的增加。这归因于药物对血脑屏障的渗透性差，导致DC在肝脏、心脏和肾脏等脑外组织中优先受到抑制。结果，血浆中多巴的浓度增加，这种氨基酸对大脑的供应也增加了。紧随其后的是脑儿茶酚胺及其代谢物酚羧酸的增加形成(Bartholini，Bates&Other，1967；Bartholini&Pletscher，1968；Bartholini，Tissot&Pletscher，1968；Constantinidis，Bartholini&Other，1968)。我们现在报告其他一些已知的DC抑制剂：MK485[~-(3，4-二羟基苯基)-a-肼-a-甲基丙酸]、NSD 101 5(间羟基苯肼)和a-甲基多巴。
Small doses of Ro 44602 [N-(~~-seryl)-N’-(2,3,4-trihydroxybenzyl)hydrazine], an inhibitor of decarboxylase (DC), enhance the dopa-induced increase of catecholamines in the brain of rats. This was attributed to a poor penetration of the drug through the blood-brain barrier leading to a preferential inhibition of DC in extracerebral tissues like liver, heart and kidney. As a consequence, the concentration of administered dopa in plasma rose and the supply to the brain of this amino-acid was enhanced. This was followed by an increased formation of cerebral catecholamines and their metabolites, the phenolic carboxylic acids (Bartholini, Bates & others, 1967 ;. Bartholini & Pletscher, 1968 ; Bartholini, Tissot & Pletscher, 1968 ; Constantinidis, Bartholini & others, 1968). We now report the effect of some other known DC inhibitors : MK485 [~-(3,4-dihydroxyphenyl)-a-hydrazino-a-methyl propionic acid] ; NSD 101 5 (m-hydroxybenzylhydrazine) and a-methyldopa.