DEPRENYL ADMINISTRATION IN MAN - SELECTIVE MONO-AMINE OXIDASE-B INHIBITOR WITHOUT CHEESE EFFECT
DEPRENYL ADMINISTRATION IN MAN - SELECTIVE MONO-AMINE OXIDASE-B INHIBITOR WITHOUT CHEESE EFFECT
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DOI：
10.1007/bf00426954
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发表时间：
1978-01-01
影响因子：
3.4
通讯作者：
KUMAR, P
中科院分区：
文献类型：
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作者：
ELSWORTH, JD;GLOVER, V;KUMAR, P
用选择性单胺氧化酶B抑制剂（-）-丙炔苯丙胺（剂量足以完全抑制血小板酶）预处理后，4名正常志愿者和6名帕金森病志愿者（2名接受L-多巴，2名接受L-多巴加卡比多巴）在口服酪胺（剂量远大于正常饮食中可能遇到的剂量）激发后未发生不良升压反应（奶酪效应）。左旋多巴-丙炔苯丙胺组合本身也不导致升压反应。正常人的肠粘膜显然主要含有对丙炔苯丙胺不敏感的A型酶，这可能会降解丙炔苯丙胺治疗志愿者中的酪胺;即使是那些长期接受药物治疗的志愿者也没有表现出奶酪效应，这表明A型酶仍然不受抑制。肠单胺氧化酶A氧化多巴胺，而在人类血小板或纹状体的胺是一个单胺氧化酶B基板。与酪胺一样，在（-）-丙炔苯丙胺治疗的受试者中，口服苯乙胺激发（剂量大于正常饮食中已知的剂量）同样未引起不良反应;其原因仍有待确定。
After pretreatment with the selective monoamine oxidase B inhibitor, (-)-deprenyl, in doses sufficient for complete inhibition of the platelet enzyme, 4 normal and 6 parkinsonian volunteers (2 receiving L-dopa and 2 L-dopa plus carbidopa) suffered no adverse pressor reaction (cheese effect) after challenge with oral tyramine in amounts considerably greater than those likely to be encountered in a normal diet. Nor did the L-dopa-deprenyl combination itself result in a pressor response. Normal human intestinal mucosa apparently predominantly contained deprenyl-insensitive A form of the enzyme, which presumably degraded administered tyramine in the deprenyl-treated volunteers; even those receiving the drug for prolonged periods manifested no cheese effect, suggesting that the A form remained uninhibited. Intestinal monoamine oxidase A oxidized dopamine, whereas in human platelet or striatum the amine was a monoamine oxidase B substrate. Like tyramine, oral phenylethylamine challenge with amounts greater than those known to be present in a normal diet similarly gave rise to no adverse reaction in (-)-deprenyl-treated subjects; the reasons for this remain to be determined.