sodium channel inhibitor 2

Sodium Channel inhibitor 2 is a blocker of sodium channel.

Valproic Acid (2-Propylpentanoic Acid) 是一种 HDAC 抑制剂，可抑制 HDAC1 活性，诱导 HDAC2 降解，具有口服活性。Valproic Acid 可以用于癫痫和躁郁症的研究。

Camostat mesylate (FOY-S980) 是口服活性合成的丝氨酸蛋白酶抑制剂，用于慢性胰腺炎。它是TMPRSS2的抑制剂，对SARS-CoV-2具有抗病毒活性。它抑制前列腺素、胰蛋白酶和苦参多糖的活性。

Eslicarbazepine Acetate (Zebinix) 是一种抗癫痫药物。Eslicarbazepine acetate 也是 β-内分泌酶(β-Secretase)和电压门控钠离子通道的双抑制剂。

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) 是动物胆汁酸的主要生物活性物质之一。它可诱导细胞凋亡，具有抗炎和免疫调节作用。

Nav1.8-IN-1 (CHEMBL1270208) 是一种有效的 Na(v)1.8 钠通道抑制剂，可用于研究精神性疼痛及炎症性疼痛。

Eslicarbazepine (Stedesa) 是口服有效抗惊厥试剂，在局部癫痫的辅助研究中具有价值。

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) 是强效的、广谱的电压门控钠通道阻滞剂，对人 Nav1.1 和 Nav1.3 亚型具有等效选择性，IC50分别为 13 nM 和 23 nM。它对Nav1.2 的抑制作用较弱，IC50为240 nM，对 Nav1.4、Nav1.6、抗TTX 的人 Nav1.5、Nav1.8 通道表现出大于 1000 倍的选择性，IC50>10 μM。

Licarbazepine (​10,11-hydroxy-10,11 Dihydrocarbamezer) 是一种有效的电压门控钠通道阻滞剂，具有抗惊厥和稳定情绪的功效。

Ceratotoxin-2 (CcoTx2) 为针对电压门控的钠通道阻滞剂，显示对Nav1.2 β1和Nav1.3 β1的强效选择性，其IC50值分别为8 nM及88 nM。

Pterinotoxin-2为一种肽类毒素，其作用机制为抑制(sodium channel)。

Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下，该化合物能够约81%地抑制Cav2.2-CRMP2相互作用，并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入（IC50约为2.8 µM）。在20 µM的浓度下，Myr-Tat-CBD3能抑制钙电流，但不影响钠电流，在初级DRG神经元中表现出这种特性。经过脊髓内给药，myr-Tat-CBD3（20 µg/5 µl）能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外，Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。

LTGO-33 是一种具有物种特异性的电压门控钠通道 NaV1.8 抑制剂，抑制 NaV1.8、 NaV1.1-NaV1.7 和 NaV1.9。LTGO-33 抑制野生型和多重 NaV1.8 与人类疼痛疾病相关的变异，可用于研究疼痛。