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Search Results for " voltage-gated sodium channels "

36

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15260	Evenamide NW-3509	Sodium Channel	Membrane transporter/Ion channel
	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。
T0939	Phenytoin 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin	Virus Protease; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	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。
T0008	Phenytoin sodium 5,5-Diphenylhydantoin sodium salt,Diphantoine,苯妥英钠,Dilantin sodium,Diphenylhydantoin Sodium	Virus Protease; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	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。
T19723	AMTB hydrochloride AMTB	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMTB hydrochloride (AMTB HCl) 是TRPM8通道的选择性阻滞剂。它抑制 icilin 诱导的 TRPM8 通道激活，pIC50为 6.23。它在膀胱过度活动和膀胱疼痛综合征中有研究的价值。它是电压门控钠通道的非选择性抑制剂 (NaV)。
T7806	Licarbazepine 10,11-hydroxy-10,11 Dihydrocarbamezer,10,11-二氢-10-羟基卡马西平	Others	Others
	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。
T9751	Transfluthrin	Others	Others
	Transfluthrin 是一种挥发性拟除虫菊酯类杀虫剂，针对昆虫电压门控钠通道 (VGSC)。
T0796	Prilocaine hydrochloride Prilocaine HCl,Propitocaine hydrochloride,Xylonest,盐酸丙胺卡因	ATPase; Sodium Channel	Membrane transporter/Ion channel
	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。
T0018	Procainamide hydrochloride Procapan,Procainamide HCl,Pronestyl,Procanbid,盐酸普鲁卡因胺	DNA Methyltransferase; Sodium Channel; AChR; Autophagy	Autophagy; Chromatin/Epigenetic; Membrane transporter/Ion channel; Neuroscience
	Procainamide hydrochloride (Procapan) 是一种用于研究心律失常的抗心律失常制剂。
T7502	PF 05089771 tosylate	Sodium Channel	Membrane transporter/Ion channel
	PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
T0222	Proparacaine hydrochloride 盐酸丙美卡因,Proparacaine HCl,Proxymetacaine Hydrochloride	Apoptosis; Sodium Channel	Apoptosis; Membrane transporter/Ion channel
	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。
T22361	Mepivacaine Carbocaine	Sodium Channel	Membrane transporter/Ion channel
	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。
T1496	Amiodarone hydrochloride 盐酸胺碘酮,Amiodar,Amiodarone HCl,Nexterone	Potassium Channel; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Amiodarone hydrochloride (Amiodarone HCl) 是一种抗心绞痛和 III 类抗心律失常药物，通过抑制钾通道和电压门控钠通道来增加心室和心房肌肉作用的持续时间，可导致心率和血管阻力降低。它通过成纤维细胞中的 ERK1/2和 p38 MAPK 信号传导诱导细胞增殖和肌成纤维细胞分化，可研究室上性和室性心律失常。
T0267	Zonisamide AD 810,唑尼沙胺,CI 912	Calcium Channel; Sodium Channel; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	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。
T13830	Propoxycaine hydrochloride	Sodium Channel	Membrane transporter/Ion channel
	Propoxycaine hydrochloride is an inhibit of voltage-gated sodium channels.
T27040	Clathrodin
	Clathrodin is a voltage-gated sodium (NaV) channels modulator.
T70224	Bupivacaine tartrate
	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.
T26564	ADCI SGB-017,SGB017,SGB 017
	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
TP1967	Phrixotoxin 3
	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.
T82700	Cn2 toxin β-Mammal toxin Cn2
	Cn2 toxin为一β类毒素，具有与电压门控钠通道（Nav）的电压感应域结合的能力。
T36813	Lu AE98134
	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].
T80185	Huwentoxin I HWTX-I	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Huwentoxin I (HWTX-I)为一种肽毒素，针对电压门控钠通道和N型钙通道具有抑制作用。该化合物对大鼠海马神经元和蟑螂DUM神经元的钠离子通道展现出抑制能力，其IC50值分别为66.1 nM和4.80 nM。
T80159	µ-Conotoxin KIIIA	Sodium Channel	Membrane transporter/Ion channel
	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。
T69145	Nisoxetine 尼索西汀
	Nisoxetine 是一种有效的和选择性的去甲肾上腺素转运蛋白(NET)抑制剂，Kd 值为 0.76 nM。Nisoxetine 是一种抗抑郁试剂和局部麻药，它可以阻断电压门控性钠通道。
T80495	mHuwentoxin-IV	Sodium Channel	Membrane transporter/Ion channel
	mHuwentoxin-IV是一种经天然修饰的Huwentoxin-IV。该化合物针对背根神经节中河豚毒素敏感(TTX-S)电压门控钠通道(sodium channels)表现出抑制作用，IC50值为54.16 nM。mHuwentoxin-IV对这些钠通道的抑制作用并不会因强去极化电压而逆转。
T82057	Iota-conotoxin RXIA
	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。
T75792	Huwentoxin XVI TFA
	Huwentoxin XVI TFA，一种来自鸟蛛 Ornithoctonus huwena 的止痛剂，一种高度可逆和选择性的哺乳动物 N 型钙通道 (N-type calcium channel) (IC50约为 60 nM) 拮抗剂。Huwentoxin XVI TFA 对电压门控的 T 型钙通道，钾通道或钠通道没有影响。
T80851	VSTx-3 Kappa-TRTX-Gr4a,κ-Theraphotoxin-Gr4a,Voltage sensor toxin 3,Peptide F
	VSTx-3是KV通道阻断剂，同时也是TTX敏感钠通道尤其是NaV1.8通道的有效阻断剂。具体而言，其对hNaV1.3通道的IC50为0.19 μM，对hNaV1.7通道的IC50为0.43 μM，对hNaV1.8通道的IC50为0.77 μM。
T80189	Hainantoxin-IV HNTX-IV	Sodium Channel	Membrane transporter/Ion channel
	Hainantoxin-IV是针对河豚毒素敏感(TTX-S)电压门控钠通道的特异性拮抗剂。该化合物以His28和Lys32为主要残基与靶标结合，并采用了抑制剂胱氨酸结基序。
T68918	Phenytoin-d10
	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...
T80426	Jingzhaotoxin-IX	Sodium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-IX是由35个氨基酸残基组成的C端酰胺化神经毒素。该化合物既抑制电压门控钠通道（包括河豚毒素抗性和河豚毒素敏感亚型）又抑制Kv2.1通道，但对延迟整流钾通道Kv1.1、1.2和1.3无效。
T35419	τ-Fluvalinate
	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 ...
T80427	Jingzhaotoxin-II	Sodium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-II是由32个氨基酸组成的神经毒素，包括两个酸性残基和两个碱性残基。该毒素能够抑制电压门控钠通道(VGSC)，并在心肌细胞上明显减缓TTX抗性(TTX-R) VGSC的快速失活，其IC50值为0.26μM。
T80491	µ-Conotoxin BuIIIB Mu-Conotoxin BuIIIB	Sodium Channel	Membrane transporter/Ion channel
	μ-Conotoxin BuIIIB (Mu-Conotoxin BuIIIB) 是一种从Cone snails毒液中分离出的肽类分子，专门抑制哺乳动物神经元的电压门控钠通道 (VGSC)，以用作研究离子通道功能的生物探针。它在神经系统疾病（例如疼痛）的研究中具有潜在应用价值。
T75855	Phrixotoxin 3 TFA
	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。
T73337	Articaine Hoe-045 free base
	Articaine (Hoe-045 free base) 是一种含酯基的酰胺类麻醉剂，可逆地与神经内腔内电压门控钠通道的α亚基结合，能有效缓解疼痛。Articaine 通过抑制NF-ĸB 的激活和NLRP3炎症小体通路改善脂多糖 (LPS) 诱导的急性肾损伤。
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...

化合物

Cat.No: T15260

Synonym: NW-3509

Target: Sodium Channel

Cat.No: T0939

Synonym: 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin

Target: Virus Protease, Sodium Channel

Phenytoin sodium

Cat.No: T0008

Synonym: 5,5-Diphenylhydantoin sodium salt,Diphantoine,苯妥英钠,Dilantin sodium,Diphenylhydantoin Sodium

Target: Virus Protease, Sodium Channel

AMTB hydrochloride

Cat.No: T19723

Synonym: AMTB

Target: TRP/TRPV Channel

Cat.No: T7806

Synonym: 10,11-hydroxy-10,11 Dihydrocarbamezer,10,11-二氢-10-羟基卡马西平

Target: Others

Cat.No: T9751

Target: Others

Prilocaine hydrochloride

Cat.No: T0796

Synonym: Prilocaine HCl,Propitocaine hydrochloride,Xylonest,盐酸丙胺卡因

Target: ATPase, Sodium Channel

Procainamide hydrochloride

Cat.No: T0018

Synonym: Procapan,Procainamide HCl,Pronestyl,Procanbid,盐酸普鲁卡因胺

Target: DNA Methyltransferase, Sodium Channel, AChR, Autophagy

PF 05089771 tosylate

Cat.No: T7502

Target: Sodium Channel

Proparacaine hydrochloride

Cat.No: T0222

Synonym: 盐酸丙美卡因,Proparacaine HCl,Proxymetacaine Hydrochloride

Target: Apoptosis, Sodium Channel

Cat.No: T22361

Synonym: Carbocaine

Target: Sodium Channel

Amiodarone hydrochloride

Cat.No: T1496

Synonym: 盐酸胺碘酮,Amiodar,Amiodarone HCl,Nexterone

Target: Potassium Channel, Adrenergic Receptor, Autophagy

Cat.No: T0267

Synonym: AD 810,唑尼沙胺,CI 912

Target: Calcium Channel, Sodium Channel, Carbonic Anhydrase

Propoxycaine hydrochloride

Cat.No: T13830

Target: Sodium Channel

Cat.No: T27040

Bupivacaine tartrate

Cat.No: T70224

Cat.No: T26564

Synonym: SGB-017,SGB017,SGB 017

Cat.No: TP1967

Cat.No: T82700

Synonym: β-Mammal toxin Cn2

Cat.No: T36813

Cat.No: T80185

Synonym: HWTX-I

Target: Calcium Channel

µ-Conotoxin KIIIA

Cat.No: T80159

Target: Sodium Channel

Cat.No: T69145

Synonym: 尼索西汀

Cat.No: T80495

Target: Sodium Channel

Iota-conotoxin RXIA

Cat.No: T82057

Huwentoxin XVI TFA

Cat.No: T75792

Cat.No: T80851

Synonym: Kappa-TRTX-Gr4a,κ-Theraphotoxin-Gr4a,Voltage sensor toxin 3,Peptide F

Cat.No: T80189

Synonym: HNTX-IV

Target: Sodium Channel

Cat.No: T68918

Jingzhaotoxin-IX

Cat.No: T80426

Target: Sodium Channel

Cat.No: T35419

Jingzhaotoxin-II

Cat.No: T80427

Target: Sodium Channel

µ-Conotoxin BuIIIB

Cat.No: T80491

Synonym: Mu-Conotoxin BuIIIB

Target: Sodium Channel

Phrixotoxin 3 TFA

Cat.No: T75855

Cat.No: T73337

Synonym: Hoe-045 free base

5α,6β-Dihydroxycholestanol

Cat.No: T37215

Cat. No.	Product Name	Target	Signaling Pathways
T2173	Veratridine	Sodium Channel	Membrane transporter/Ion channel
	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。
TN1254	3'-Methoxydaidzein 3'-甲氧基大豆苷元	Sodium Channel	Membrane transporter/Ion channel
	3'-Methoxydaidzein 是一种异黄酮和 Sodium Channel 双重抑制剂。3'-Methoxydaidzein 对NaV1.7、NaV1.8 和 NaV1.3有抑制作用，IC50 分别为 181 nM、397 nM 和 505 nM。 3'-Methoxydaidzein 对胶原诱导的血小板聚集具有特异性，IC50值分别为12.3和61.5µM。。3'-Methoxydaidzein 通过抑制电压门控钠通道发挥镇痛作用。 3'-Methoxydaidzein 具有抗氧化活性和抗血小板聚集活性。
T36068	Brevetoxin B
	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.

天然产物

Cat.No: T2173

Target: Sodium Channel

3'-Methoxydaidzein

Cat.No: TN1254

Synonym: 3'-甲氧基大豆苷元

Target: Sodium Channel

Cat.No: T36068

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