TETRAHYDRO‐β‐CARBOLINES: SPECIFIC INHIBITORS OF TYPE A MONOAMINE OXIDASE IN RAT BRAIN 1
TETRAHYDRO‐β‐CARBOLINES: SPECIFIC INHIBITORS OF TYPE A MONOAMINE OXIDASE IN RAT BRAIN 1
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四氢-β-咔啉：大鼠脑中 A 型单胺氧化酶的特异性抑制剂 1
DOI：
10.1111/j.1471-4159.1977.tb10661.x
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发表时间：
1977
影响因子：
4.7
通讯作者：
A. Friedhoff
中科院分区：
文献类型：
--
作者：
E. Meller;E. Friedman;J. Schweitzer;A. Friedhoff
摘要-测试了一系列5-羟色胺和苯乙胺类似物对大鼠下丘脑中A型或B型单胺氧化酶（EC 1.4.3.4）的差异抑制能力。几种四氢-β-咔啉显示出最具特异性和效力的作用，它们在微摩尔浓度下竞争性抑制5-羟色胺的氧化脱氨基作用。与此相反，有效抑制苯乙胺脱氨基作用，观察到只有在或接近毫摩尔浓度的这些药物。在25-100 mg/kg（i. p.）给药后，也观察到A型MA 0活性显著降低，但B型MA 0活性未显著降低，四氢β咔啉及其6甲氧基衍生物
Abstract— A series of serotonin and phenethylamine analogs were tested for their ability to differentially inhibit type A or B monoamine oxidase (EC 1.4.3.4) in rat hypothalamus. The most specific and potent effects were shown by several tetrahydro‐β‐carbolines which competitively inhibited the oxidative deamination of serotonin at micromolar concentrations. In contrast, effective inhibition of phenethylamine deamination was observed only at or near millimolar concentrations of these drugs. Significant reductions of type A but not type B MA0 activity were also observed after administration of 25–100 mg/kg, i.p., of tetrahydro‐β‐carboline and its 6‐methoxy derivative.