Huang Yu-Yin, Liu Yu-Chao, Lee Cheng-Ta, Lin Yen-Chu, Wang Mong-Lien, Yang Yi-Ping, Chang Kaung-Yi, Chiou Shih-Hwa
Institute of Clinical Medicine, National Yang-Ming University, Taipei 112, Taiwan.
Department of Anesthesiology, Cheng Hsin General Hospital, Taipei 112, Taiwan.
Int J Mol Sci. 2016 Jul 22;17(7):1191. doi: 10.3390/ijms17071191.
Lamotrigine (LTG) is generally considered as a voltage-gated sodium (Nav) channel blocker. However, recent studies suggest that LTG can also serve as a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel enhancer and can increase the excitability of GABAergic interneurons (INs). Perisomatic inhibitory INs, predominantly fast-spiking basket cells (BCs), powerfully inhibit granule cells (GCs) in the hippocampal dentate gyrus. Notably, BCs express abundant Nav channels and HCN channels, both of which are able to support sustained action potential generation. Using whole-cell recording in rat hippocampal slices, we investigated the net LTG effect on BC output. We showed that bath application of LTG significantly decreased the amplitude of evoked compound inhibitory postsynaptic currents (IPSCs) in GCs. In contrast, simultaneous paired recordings from BCs to GCs showed that LTG had no effect on both the amplitude and the paired-pulse ratio of the unitary IPSCs, suggesting that LTG did not affect GABA release, though it suppressed cell excitability. In line with this, LTG decreased spontaneous IPSC (sIPSC) frequency, but not miniature IPSC frequency. When re-examining the LTG effect on GABAergic transmission in the cornus ammonis region 1 (CA1) area, we found that LTG markedly inhibits both the excitability of dendrite-targeting INs in the stratum oriens and the concurrent sIPSCs recorded on their targeting pyramidal cells (PCs) without significant hyperpolarization-activated current (Ih) enhancement. In summary, LTG has no effect on augmenting Ih in GABAergic INs and does not promote GABAergic inhibitory output. The antiepileptic effect of LTG is likely through Nav channel inhibition and the suppression of global neuronal network activity.
拉莫三嗪(LTG)通常被认为是一种电压门控钠(Nav)通道阻滞剂。然而,最近的研究表明,LTG还可作为超极化激活的环核苷酸门控(HCN)通道增强剂,并可增加γ-氨基丁酸能中间神经元(INs)的兴奋性。躯体周围抑制性INs,主要是快速放电篮状细胞(BCs),能有力地抑制海马齿状回中的颗粒细胞(GCs)。值得注意的是,BCs表达丰富的Nav通道和HCN通道,这两种通道都能够支持持续动作电位的产生。我们使用大鼠海马脑片的全细胞记录技术,研究了LTG对BC输出的净效应。我们发现,浴加LTG可显著降低GCs中诱发的复合抑制性突触后电流(IPSCs)的幅度。相比之下,从BCs到GCs的同步配对记录显示,LTG对单位IPSCs的幅度和配对脉冲比率均无影响,这表明LTG虽抑制细胞兴奋性,但不影响γ-氨基丁酸(GABA)的释放。与此一致的是,LTG降低了自发性IPSC(sIPSC)频率,但未降低微小IPSC频率。当重新研究LTG对海马杏仁核区1(CA1)区域GABA能传递的影响时,我们发现LTG显著抑制了海马下托中靶向树突的INs的兴奋性以及在其靶向锥体细胞(PCs)上记录到的同步sIPSCs,且未显著增强超极化激活电流(Ih)。总之,LTG对增强GABA能INs中的Ih无作用,也不促进GABA能抑制输出。LTG的抗癫痫作用可能是通过抑制Nav通道和抑制整体神经元网络活动实现的。