voltage-gated na+ channel

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。

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。

Benzocaine xHCl(94-09-7(free base)) 与电压门控 Na+ 通道中的所有其他 rLA 共享一个共同受体（测试的 IC50 为 0.8 mM，电位为 +30 mV）。

Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator. Brevetoxin-3 has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels.

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。

Sodium Channel inhibitor1 is a novel and selective voltage-gated sodium channel for pain treatment. (IC50 Value of 0.16 uM and 0.41 uM for Na v1.7, V hold-90mV and Na v1.7, V hold-90mV)

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。

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。

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。

QAQ dichloride is a photoswitchable compound that blocks voltage-gated Na v and K v channels. Its channel-blocking activity is observed in the trans form of the azobenzene photoswitch, while the cis form does not exhibit this effect. This compound is membrane-impermeant and selectively enters pain-sensing neurons expressing endogenous import channels. QAQ dichloride functions as a light-sensitive analgesic and provides a valuable tool for investigating signaling mechanisms involved in acute and chronic pain [1] [2].

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。

Bupivacaine is a BK SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM 40% & 20 μM 60% at pH 9.0, 5 nM 28% & 3 μM 72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM 39% & 10 μM 61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1 2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

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。

Nav1.3 channel inhibitor 1 (化合物 15b) 为状态依赖性电压门控钠通道Nav1.3的抑制剂，具有IC50值为20 nM。该化合物能穿透血脑屏障，适用于神经系统疾病研究。

ProTx-III是一种从秘鲁绿绒狼蛛毒液中分离得到的蜘蛛毒肽，它是一个选择性且有效的Nav1.7电压门控钠离子通道抑制剂，其IC50值为2.1 nM。ProTx-III特征为含有典型的抑制剂胱氨酸结基序(ICK)，并可逆转疼痛反应，适用于慢性疼痛、癫痫和心律失常等疾病的研究。

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。

Kurtoxin是一种选择性Cav3 (T-type) 电压门控Ca2+通道抑制剂，对Cav3.1 (α1G T-type) Ca2+通道的Kd值为15 nM。该化合物与中枢和外周神经元的L型、N型和P型Ca2+通道有高度亲和性，并对电压门控Na+通道也有交叉反应性。