正乙酰基-6-氨基己酸化合物可抑制神经纤维传导性

Mazov Y.A., Dmitriev A.A., Pirozhkov A.S., Blinov D.S., Timoshkin D.E., Turmulaeva R.M., S. E.V., B. E.V.
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引用次数: 0

摘要

研究了纯度为 99.8%的 N-乙酰基-6-氨基己酸盐(化合物 LHT-9-17)的局部麻醉效果,还评估了该物质在正常 pH 值和酸中毒背景下对单个钠通道电导率和神经导体电导率的影响。在病理发展的第 12 天,评估了通过眶下给药诱导的 2% LHT-9-17 和 2% 盐酸利多卡因溶液的局部麻醉效果。通过膜片钳法评估了离体大鲵神经元单个Na-通道的传导情况。在含有 0.00001 至 0.01 μM LCT-9-17 的灌注室中对桡骨蛙离体坐骨神经的动作电位进行了登记。实验包括增加刺激强度,直至达到最大反应。化合物 LHT-9-17 具有局部麻醉活性,包括在炎症过程中。镇痛效果是由于抑制了神经导体 Na 通道的传导性。在炎症条件下保持活性可能是由于物质对炎症状态的作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
N-ACETYL-6-AMINOHEXANOIC ACID COMPOUND INHIBITS NERVE FIBERS CONDUCTIVITY
Local anesthetic effect of N-acetyl-6-aminohexanoate salt (compound LHT-9-17) in the form of a substance with a purity of 99.8% was studied and also assessed the effect of the substance on the conductivity of single sodium channels and the conductivity of the nerve conductor at normal pH values and against the background of acidosis. Experimental ligature periodontitis was modeled in 20 laboratories male Wistar rats weighing 200-220 g. Local anesthetic effects of 2% LHT-9-17 and 2% lidocaine hydrochloride solution induced by infraorbital administration was assessed at day 12 of the pathology development. Conduction of single Na-channels was assessed by patch-clamp method on isolated giant neurons of Limnea stagnalis. Registration of the action potential of Rana radibunda isolated sciatic nerve was carried out in perfusion chamber contained 0.00001 to 0.01 μM LCT-9-17. Experiments included increasing the force of stimulating incentives until the maximum response. Compound LHT-9-17 has local anesthetic activity, including during the inflammatory process. The analgesic effect is due to the suppression of the conductivity of Na-channels of nerve conductors. The activity kept under inflammatory conditions may be due to the action of substances against the inflammatory state.
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