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The effect of N-methyl-norsalsolinol on monoamine oxidase of the rat caudate nucleus in vitro.

机译:N-甲基-norsalsolinol在体外对大鼠尾状核单胺氧化酶的影响。

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摘要

The effects of N-methyl-norsalsolinol on basal and inhibited activity of monoamine oxidase (MAO) in membrane preparations from the caudate nucleus of the rat have been studied. For the first time, the physiological step of dopamine oxidation to 3, 4 dihydroxyphenylacetic aldehyde (DPAA) was examined. N-methyl-norsalsolinol (2-MDTIQ) dose-dependently inhibited MAO activity with a IC50 of 33 microM. The MAO inhibitors clorgyline and deprenyl were also found to inhibit formation of DPAA. In this case, the inhibition of these antagonists, clorgyline and deprenyl, was additive. N-methyl-norsalsolinol modified neither the enzyme inhibition induced by clorgyline nor by deprenyl. These results suggest that 2-MDTIQ, the naturally occurring compound found in parkinsonian brain and cerebrospinal fluid, perturbs dopamine metabolism in basal ganglia.
机译:研究了N-甲基-降冰片烯醇对大鼠尾状核膜制剂中单胺氧化酶(MAO)的基础和抑制活性的影响。首次检查了多巴胺氧化为3,4二羟基苯基乙醛(DPAA)的生理步骤。 N-甲基-norsalsolinol(2-MDTIQ)剂量依赖性地抑制MAO活性,IC50为33 microM。还发现了MAO抑制剂clorgyline和deprenyl抑制DPAA的形成。在这种情况下,对这些拮抗剂克古林和去异戊二烯的抑制作用是累加的。 N-甲基-norsalsolinol既不修饰高铁碱也不抑制异戊二烯基诱导的酶抑制作用。这些结果表明2-MDTIQ是在帕金森氏症的大脑和脑脊液中发现的天然化合物,扰乱了基底神经节中的多巴胺代谢。

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