托吡酯抑制高原的起始电位令人沮丧的异形战机在CA1神经细胞钙通道。

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Kuzmiski JB,巴尔W, Zamponi GW, MacVicar英航

托吡酯抑制高原的起始电位令人沮丧的异形战机在CA1神经细胞钙通道。

Epilepsia。2005年4月,46 (4):481 - 9。doi: 10.1111 / j.0013-9580.2005.35304.x。

PubMed ID

15816941 (在PubMed

]

文摘

目的:Cholinergic-dependent高原势(PPs)本质上产生电导可以引出ictal-type癫痫活动。本研究的目的是探讨托吡酯(TPM)的行为在PPs的一代。方法:我们用全细胞膜片箝记录在大鼠海马CA1锥体神经元片检查对PPs TPM的影响。结果:在current-clamp模式下,动作电位诱发PPs后胆碱能受体刺激。治疗相关的浓度TPM (50 microM)沮丧的PPs诱发动作电位。令人惊讶的是,在电压钳模式中,我们发现循环nucleotide-gated (CNG)目前是PP代(表示我(尾巴))并不沮丧。然而,大大延长去极化电压的步骤是需要引起我(尾巴)。这表明钙进入触发唤起PPs被TPM沮丧,而不是我(尾巴)本身。TPM没有影响钙峰值控制条件;然而,TPM并减少钙cholinergic-receptor刺激后峰值。 We recently found that R-type calcium spikes are enhanced by cholinergic-receptor stimulation. Therefore we isolated R-type calcium spikes with a cocktail containing tetrodotoxin, omega-conotoxin MVIIC, omega-conotoxin-GVIA, omega-agatoxin IVA, and nifedipine. R-type calcium spikes were significantly depressed by TPM. We also examined the effects of TPM on recombinant Ca(V)2.3 calcium channels expressed in tsA-201 cells. TPM depressed currents mediated by Ca(V)2.3 subunits by a hyperpolarizing shift in steady-state inactivation. CONCLUSIONS: We have found that TPM reduces ictal-like activity in CA1 hippocampal neurons through a novel inhibitory action of R-type calcium channels.

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药物靶点

药物	目标	类	生物	药理作用	行动
托吡酯	压敏电阻器异形战机钙通道(蛋白质组)	蛋白质组	人类	未知的	拮抗剂	细节