voltage-gated sodium channels

Veratridine 是一种生物碱，来自百合科植物。Veratridine 是一种钠通道激动剂， 对 Nav1.7 的峰值电流具有抑制作用，IC50为 18.39 µM。

Phenytoin sodium (Diphantoine) 是一种有效的电压门控钠离子通道阻滞剂，可减少小鼠乳腺肿瘤的生长和转移，具有抗癫痫活性。

Procainamide hydrochloride (Procapan) 是一种用于研究心律失常的抗心律失常制剂。

Proparacaine hydrochloride (Proparacaine HCl) 是 Lidocaine 的衍生物，具有糖皮质激素样活性和免疫调节作用。

Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。

Prilocaine hydrochloride (Prilocaine HCl) 是一种氨基酰胺类局部麻醉剂，作用于神经元膜上的钠通道并限制癫痫发作的扩散。它是Na K-ATPase 抑制剂，具有神经毒性作用。

Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控钠离子通道阻滞剂，可减少小鼠乳腺肿瘤的生长和转移，具有抗癫痫活性。

Mexiletine hydrochloride (KOE-1173 hydrochloride) 是一种电压门控钠通道阻滞剂，是 IB 类抗心律失常药。 Mexiletine hydrochloride 通过抑制心肌细胞内钠电流，从而降低心脏动作电位（0相）上升速率，并且降低浦肯野纤维的自律性而发挥抗心律失常作用。

Amiodarone hydrochloride（盐酸胺碘酮）是一种抗心绞痛药物和 III 类抗心律失常剂，可抑制钾通道（包括野生型 IhERG 钾通道及其尾电流，IC₅₀ 约为 45 nM）以及电压门控钠通道，从而延长心室和心房肌肉的动作电位持续时间，降低心率和血管阻力。它通过激活成纤维细胞中的 ERK1/2 和 p38 MAPK 信号通路，诱导细胞增殖和肌成纤维细胞分化，广泛用于室上性和室性心律失常的研究，并可用于构建肺纤维化动物模型。

Mepivacaine (Carbocaine) 是一种可用于局部麻醉的酰胺类化合物，可使人或动物短暂的失去自知觉。Mepivacaine 通过与神经细胞膜上特定的电压门控钠离子通道结合，抑制钠离子内流和膜去极化来发挥作用。Mepivacaine 适用于神经阻滞和硬膜外麻醉。

RY785 是电压门控钾 (KV2)通道的选择性抑制剂， KV2.2 的 IC50为 0.05 μM。它在缓解疼痛方面具有研究价值。

Propoxycaine hydrochloride 是一种酯类局部麻醉剂，抑制电压门控的钠通道，可调节神经冲动，可诱导感觉丧失。Propoxycaine hydrochloride 可调节SPMVs脂质双层的流动。

Evenamide (NW-3509) 是一种口服有效的电压门控钠通道 (sodium channel, VGSC) 阻滞剂，Ki 为 0.4 µM，在精神分裂症中有研究价值。Evenamide 在精神病，躁狂症，抑郁和攻击性的各种啮齿动物模型中具有显著功效。

Lubeluzole (dihydrochloride) 是一种神经保护剂，主要通过阻断神经元电压门控钠通道 (sodium channels) 来发挥作用。此外，它对心脏钠通道 (sodium channels) 也具有持续的抑制效果，使其在抗心律失常试剂研究中显示出潜在应用价值。

Insecticidal agent 21 (Compound 6) 是一种有效针对Culex pipiens幼虫的杀虫剂 (LC50: 0.4 μg/mL)。其通过抑制乙酰胆碱酯酶 (AChE) 并同时作用于其他神经受体，包括烟碱乙酰胆碱受体 (nAChR)、电压门控钠通道 (VGSC) 和 γ-氨基丁酸受体 (GABAAR)，从而实现多靶点神经毒性。Insecticidal agent 21显示出卓越的杀虫性能，可用于开发新型杀虫剂，以应对蚊虫对传统药剂的抗药性。

(R)-(+)-Bupivacaine hydrochloride 是一种电压门控钠通道 (sodium channel) 抑制剂，通过选择性阻断神经细胞膜上的电压门控钠离子通道，抑制钠离子内流，从而干扰神经冲动的产生与传导，实现局部麻醉效果。此化合物适用于急性疼痛的研究。

Co 102862 是一种电压门控钠通道阻滞剂。 Co 102862 可用于抗惊厥的研究。

ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and o

Clathrodin is a voltage-gated sodium (NaV) channels modulator.

DPI 201-106对电压门控钠通道的有心脏选择性调节活性，从而产生正性肌力作用。DPI 201-106 具有协同肌膜和细胞内作用机制。

τ-Fluvalinate is a pyrethroid acaricide.1It induces tail currents in Western honeybee (A. mellifera) voltage-gated sodium channels (AmNav1) expressed inXenopusoocytes (EC50= 60 nM). It also induces tail currents in honeybee parasitic Varroa mite (V. destructor) Nav1 channels (VdNav1) expressed inXenopusoocytes (EC50= 160 nM) with a faster tail current decay than that of AmNav1 channels. Topical application of τ-fluvalinate (2 μl) in combination with coumaphos , atrazine , 2,4-DMPF, chlorpyrifos , and chlorothalonil does not affect honeybee queen mass, egg-laying patterns, or the mass of daughter worker bees at emergence.2Formulations containing τ-fluvalinate have been used to control Varroa mites in beehives. 1.Gosselin-Badaroudine, P., and Chahine, M.Biophysical characterization of the Varroa destructor NaV1 sodium channel and its affinity for τ-fluvalinate insecticideFASEB J.31(7)3066-3071(2017) 2.McAfee, A.Honey bee queen health is unaffected by contact exposure to pesticides commonly found in beeswaxSci. Rep.11(1)15151(2021)

Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal slices. It protects against seizures induced by maximal electroshock (MES) in mice. Formulations containing phenytoin have been used in the treatment of tonic-clonic seizures and status epilepticus.