作者: Zdeněk Fišar , Jana Hroudová , Jan Korábečný , Kamil Musílek , Kamil Kuča
DOI: 10.1016/J.TOXLET.2010.12.023
关键词:
摘要: Abstract Administration of acetylcholinesterase (AChE) reactivators (oximes) is usually used in order to counteract the poisoning effects nerve agents. The possibility was suggested that oximes may show some therapeutic and/or adverse through their action central nervous system. There are no sufficient data about interaction with monoaminergic neurotransmitter's systems brain. Oxime-type AChE pralidoxime, obidoxime, trimedoxime, methoxime and HI-6 were tested for potential affect activity monoamine oxidase type A (MAO-A) B (MAO-B) crude mitochondrial fraction pig brains. compounds found inhibit fully MAO-A half maximal inhibitory concentration (IC50) 0.375 mmol/l (pralidoxime), 1.53 mmol/l (HI-6), 2.31 mmol/l (methoxime), 2.42 mmol/l (obidoxime) 4.98 mmol/l (trimedoxime). Activity MAO-B inhibited by pralidoxime only IC50 4.81 mmol/l 11.01 mmol/l, respectively. Methoxime, obidoxime trimedoxime displayed non-monotonic dependent effect on activity. Because concentrations effective MAO inhibition could not be achieved vivo at cerebral level, we suppose investigated do interfere brain therapeutically relevant concentrations.