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首页> 外文期刊>International Journal of Environmental Research and Public Health >6 Hz Active Anticonvulsant Fluorinated N-Benzamide Enaminones and Their Inhibitory Neuronal Activity
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6 Hz Active Anticonvulsant Fluorinated N-Benzamide Enaminones and Their Inhibitory Neuronal Activity

机译：6 Hz主动抗惊厥氟化N-苯甲酰胺烯酮及其抑制神经元活性

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摘要

A small library of novel fluorinated N-benzamide enaminones were synthesized and evaluated in a battery of acute preclinical seizure models. Three compounds (GSA 62, TTA 35, and WWB 67) were found to have good anticonvulsant activity in the 6-Hz ‘psychomotor’ 44-mA rodent model. The focus of this study was to elucidate the active analogs’ mode of action on seizure-related molecular targets. Electrophysiology studies were employed to evaluate the compounds’ ability to inhibit neuronal activity in central olfactory neurons, mitral cells, and sensory-like ND7/23 cells, which express an assortment of voltage and ligand-gated ion channels. We did not find any significant effects of the three compounds on action potential generation in mitral cells. The treatment of ND7/23 cells with 50 μM of GSA 62, TTA 35, and WWB 67 generated a significant reduction in the amplitude of whole-cell sodium currents. Similar treatment of ND7/23 cells with these compounds had no effect on T-type calcium currents, indicating that fluorinated N-benzamide enaminone analogs may have a selective effect on voltage-gated sodium channels, but not calcium channels.
机译：合成了一个小型的新型氟化N-苯甲酰胺烯胺类文库，并在一系列急性临床前癫痫发作模型中进行了评估。在6 Hz的“精神运动” 44 mA啮齿动物模型中，发现三种化合物（GSA 62，TTA 35和WWB 67）具有良好的抗惊厥活性。这项研究的重点是阐明活性类似物对癫痫相关分子靶标的作用方式。电生理学研究用于评估该化合物抑制中枢嗅觉神经元，二尖瓣细胞和感觉样ND7 / 23细胞（表达电压和配体门控离子通道的种类）中神经元活性的能力。我们没有发现这三种化合物对二尖瓣细胞产生动作电位有任何显着影响。用50μM的GSA 62，TTA 35和WWB 67处理ND7 / 23细胞可显着降低全细胞钠电流的幅度。用这些化合物对ND7 / 23细胞进行相似的处理对T型钙电流没有影响，表明氟化的N-苯甲酰胺烯胺酮类似物可能对电压门控的钠通道有选择性的作用，但对钙通道没有影响。

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