nav1.2

NaV1.2/1.6 channel blocker-1 是一种有效的 NaV1.2/1.6 channel 阻滞剂，对 rNaV1.6 和 hNaV1.2 有抑制作用。NaV1.2/1.6 channel blocker-1 可用于研究全身性癫痫和运动障碍。

Nav1.2-IN-1 (compound 5i) 是一种 3-(1,2,3,6-tetrahydropyridine)-4-azaindole 衍生物，具高效性和选择性，可作为 Nav1.2 的抑制剂。该化合物能降低 Nav1.2 电流峰值，IC50 值为 7.79 μM，并展现抗癫痫活性。在皮下注射戊四氮 (sc-PTZ) 诱发的癫痫模型中，它展现出优异的抗惊厥效果且神经毒性低。

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor (Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7) for the treatment of chronic pain.

XPC-6444 is a isoform-selective, and CNS-penetrant inhibitor of NaV1.6 with IC50 of41 nM for hNaV1.6,with anticonvulsant activity.

Anticonvulsant agent 9 (compound 4f) 是一种 α1β2γ2GABAA受体激活剂，其EC50为1.24 μM。该化合物激活α1β2γ2GABAA受体并抑制Nav1.2通道的失活，表现出显著的抗惊厥活性。

Photoswitchable Kv channel blocker (IC50 values are 2 and 64 μM at 500 nm and 380 nm respectively). Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Exhibits minimal activity at Nav1.2 and L-type Ca2+ channels. Stimulates action potential firing of hippocampal neurons in vitro at 500 nm and restores visual responsiveness in blind mice at 380 nm. Fortin et al (2008) Photochemical control of endogenous ion channels and cellular excitability. Nat.Methods 5 331 PMID:18311146 |Polosukhina et al (2012) Photochemical restoration of visual responses in blind mice. Neuron 75 271 PMID:22841312 |Banghart et al (2009) Photochromic blockers of voltage-gated potassium channels. Angew.Chem.Int.Ed. 48 9097 PMID:19882609

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].

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

GDC-0310是一种选择性和可口服的Nav1.7抑制剂，对人Nav1.7的IC50=0.6 nM，可用于研究疼痛。

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).

AA43279 is a novel selective Nav1.1 activator, increasing the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increasing the spontaneous inhibitory post-synaptic currents (sIPSCs) recorded from pyramidal neurons.

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。

Phrixotoxin 3 TFA 是一种高效的电压门控钠通道阻滞剂，对NaV1.2、NaV1.3、NaV1.4、NaV1.1及NaV1.5的IC50值分别为0.6、42、72、288和610 nM。该化合物通过改变门控动力学的去极化并阻断钠电流的内向流，调控电压门控钠通道，表现出类似典型门控修饰毒素的作用机制。

Huwentoxin-IV TFA是一种具有高效性和选择性的钠通道阻滞剂，能够抑制Nav1.7、Nav1.2、Nav1.3和Nav1.4神经元，其IC50分别为26、150、338和400nM。通过优先结合于神经毒素受体位点4，Huwentoxin-IV TFA特异性地阻断周围神经的Nav1.7亚型。该化合物适用于炎症性及神经性疼痛动物模型的研究。

μ-Conotoxin KIIIA，一种具有镇痛功能的μ-芋螺毒素，源自Conus kinoshitai。该化合物通过阻断哺乳动物神经元的电压门控钠通道(VGSC) (Nav1.2)，可应用于疼痛研究领域。

GrTx1是一种从Grammostola rosea蜘蛛的毒液中分离的肽毒素。该分子能够阻断sodium channel，对Nav1.1，Nav1.2，Nav1.3，Nav1.4，Nav1.6和Nav1.7具有不同的抑制作用，IC50值分别为0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM和0.37 µM，适用于神经疾病的研究领域。

GsAF-I是Nav和hERG1通道的有效阻滞剂，其IC50值针对Nav1.1、Nav1.2、Nav1.3、Nav1.4、Nav1.6、Nav1.7和hERG1分别为0.36μM、0.6μM、1.28μM、0.33μM、1.2μM、0.04μM和4.8μM。

Phlo1b（μ-TrTx-Phlo1b）为含35个氨基酸残基的肽毒素，特异性抑制Nav1.7通道。相较之下，其对Nav1.2与Nav1.5的抑制作用较弱。

Phlo1a（μ-TrTx-Phlo1a）是含35个氨基酸残基的肽类毒素。Phlo1b为选择性Nav1.7抑制剂，而Phlo1a对Nav1.2与Nav1.5显示较低的抑制活性。

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。

Ceratotoxin-1 (CcoTx1)为电压门控钠通道亚型的抑制剂，特别是对Nav1.1/β1、Nav1.2/β1、Nav1.4/β1和Nav1.5/β1具有不同程度的抑制效果，其IC50值分别为523 nM、3 nM、888 nM和323 nM。此外，Ceratotoxin-1对Nav1.8/β1亦有抑制作用。

Iota-conotoxin RXIA是一种作用于电压门控钠通道（Nav1.2, 1.6, 1.7）的激动剂，其在小鼠脑内注射后能够引发青蛙运动神经轴突的重复动作电位以及癫痫样发作。

XPC-5462是NaV1.6和NaV1.2抑制剂，其IC50s分别为10.9 nM和10.3 nM。XPC-5462在离体脑切片发作模型中抑制癫痫样活动。

Potent blocker of voltage-gated sodium channels (IC50 values are 0.6, 42, and 72 nM for NaV1.2, NaV1.3 and NaV1.5 respectively). Blocks inward sodium currents in a voltage-dependent manner.