Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
J Pharmacol Sci. 2018 May;137(1):93-97. doi: 10.1016/j.jphs.2018.01.010. Epub 2018 Mar 30.
The neurosteroid allopregnanolone has potent analgesic effects, and its potential use for neuropathic pain is supported by recent reports. However, the analgesic mechanisms are obscure. The voltage-gated sodium channels (Na) α subunit Na1.3 is thought to play an essential role in neuropathic pain. Here, we report the effects of allopregnanolone sulfate (APAS) on sodium currents (I) in Xenopus oocytes expressing Na1.3 with β or β subunits. APAS suppressed I of Na1.3 with β and β in a concentration-dependent manner (IC values; 75 and 26 μmol/L). These results suggest the possible importance of Na1.3 inhibition for the analgesic mechanisms of allopregnanolone.
神经甾体孕烷醇酮具有很强的镇痛作用，最近的报道支持其用于治疗神经性疼痛。然而，其镇痛机制尚不清楚。电压门控钠离子通道（Na）α亚基 Na1.3 被认为在神经性疼痛中起重要作用。在这里，我们报告了孕烷醇酮硫酸盐（APAS）对表达 Na1.3 的非洲爪蟾卵母细胞中钠离子电流（I）的影响，这些 Na1.3 与β或β亚基一起表达。APAS 以浓度依赖的方式抑制 Na1.3 与β和β的 I（IC 值分别为 75 和 26 μmol/L）。这些结果表明 Na1.3 抑制可能是孕烷醇酮镇痛机制的重要因素。
