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The effects of huwentoxin-I on the voltage-gated sodium channels of rat hippocampal and cockroach dorsal unpaired median neurons

机译:huwentoxin-I对大鼠海马和蟑螂背侧未配对正中神经元电压门控钠通道的影响

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摘要

Huwentoxin-I (HWTX-I) is a 33-residue peptide isolated from the venom of Ornithoctonus huwena and could inhibit TTX-sensitive voltage-gated sodium channels and N-type calcium channels in mammalian dorsal root ganglion (DRG) neurons. However, the effects of HWTX-I on mammalian central neuronal and insect sodium channel subtypes remain unknown. In this study, we found that HWTX-I potently inhibited sodium channels in rat hippocampal and cockroach dorsal unpaired median (DUM) neurons with the IC 50 values of 66.1 ± 5.2 and 4.80 ± 0.58 nM, respectively. Taken together with our previous work on DRG neurons (IC 50 ≈ 55 nM), the order of sodium channel sensitivity to HWTX-I inhibition was insect central DUM mammalian peripheral mammalian central neurons. HWTX-I exhibited no effect on the steady-state activation and inactivation of sodium channels in rat hippocampal and cockroach DUM neurons.
机译:Huwentoxin-I(HWTX-1)是从Ornithoctonus huwena的毒液中分离的33个残基肽,可以抑制哺乳动物背根神经节(DRG)神经元中的TTX敏感电压门控钠通道和N型钙通道。然而,HWTX-1对哺乳动物中枢神经元和昆虫钠通道亚型的影响仍然未知。在这项研究中,我们发现HWTX-1可以有效抑制大鼠海马和蟑螂背侧非配对中位(DUM)神经元的钠通道,其IC 50值分别为66.1±5.2和4.80±0.58 nM。与我们先前对DRG神经元的研究(IC 50≈55 nM)一起,钠通道对HWTX-1抑制的敏感性顺序是昆虫中枢DUM哺乳动物外围>哺乳动物中枢神经元。 HWTX-1对大鼠海马和蟑螂DUM神经元的稳态激活和钠通道失活没有影响。

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