Sodium Channel

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抑制剂选择性比较

Sodium Channel产品

所有产品(57) Sodium Channel抑制剂(54) Sodium Channel激活剂(1) Sodium Channel拮抗剂(2)

目录号	产品描述	文献引用	实验数据
S1614	Riluzole Riluzole (RP-54274, PK 26124) 是谷氨酸盐释放抑制剂，具有神经保护、抗癫痫、抗焦虑以及麻醉作用。	Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183 J Cell Biochem, 2019, 10.1002/jcb.29533	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S2454	Bupivacaine HCl Bupivacaine HCl 可以与钠离子通道的胞内部分结合从而阻断进入神经细胞的钠离子流，用于治疗心律不齐。	Int J Mol Sci, 2019, 20(17) J Steroid Biochem Mol Biol, 2017, 172:89-97 Breast Cancer Res Treat, 2015, 150(3):535-45
S1811	Amiloride HCl Amiloride是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。	Signal Transduct Target Ther, 2020, 5(1):214 PLoS Genet, 2020, 16(10):e1009100 Drug Discov Ther, 2020, 14(5):256-258
S1256	Rufinamide Rufinamide (CGP 33101)是一种电压门控式的sodium channel阻断剂，用作抗惊厥的药物。
S1603	Furosemide Furosemide 是一种有效的NKCC2抑制剂，用于治疗充血性心脏衰竭和水肿。	Sci Rep, 2018, 8(1):9302 Biomed Pharmacother, 2018, 101:145-154 Vascul Pharmacol, 2017, 99:74-82
S6920^New	SEA0400 SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂，可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收，对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERK 和 p38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。
S4339^New	Meticrane Meticrane 是一种利尿剂，可抑制远曲小管中 reabsorption of sodium and chloride ions 的重吸收。Meticrane 可用于治疗原发性高血压。
S0016^New	SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3，对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
S1445	Zonisamide Zonisamide (CI-912)是FDA批准的抗癫痫药物，阻断电压依赖性钠（+）通道和T型钙离子通道。
S2524	Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin)是一种失活的电压门控钠离子通道稳定剂。
S1693	Carbamazepine Carbamazepine (Carbatrol, NSC 169864) 是一种钠离子通道抑制剂，作用于大鼠脑突触体时， IC50为131 μM。	PLoS One, 2019, 14(2):e0211644 DNA Cell Biol, 2019, 10.1089/dna.2018.4553
S2785	A-803467 A-803467是一种选择性Na_V1.8 channel抑制剂，IC50为8 nM，抑制抗河豚毒的电流，比作用于人类Na_V1.2， Na_V1.3， Na_V1.5和Na_V1.7选择性高100倍以上。
S2560	Amiloride HCl dihydrate Amiloride HCl dihydrate是一种有效的上皮细胞钠离子通道抑制剂。	PLoS Genet, 2020, 16(10):e1009100 Sci Rep, 2017, 7(1):5586 Peptides, 2015, 73:67-76
S1287	Bumetanide Bumetanide是一种氨磺酰基类的袢利尿剂，用于治疗心脏衰竭。	Cell Mol Gastroenterol Hepatol, 2019, 10.1016/j
S2525	Phenytoin Phenytoin (Diphenylhydantoin) 是一种失活的电压门控钠离子通道稳定剂。
S2874	Camostat Mesilate Camostat (FOY-305)是胰蛋白酶样的蛋白酶抑制剂，抑制上皮细胞钠离子通道(ENaC)功能，IC50为50 nM, 对Trypsin, Prostasin 和 Matriptase作用效果稍弱。	EMBO J, 2020, e2020106057 Sci Immunol, 2020, 13;5(47):eabc3582 bioRxiv, 2020, 2020.11.04.364315
S2114	Dronedarone HCl Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。	Cell Syst, 2019, 8(2):97-108 Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
S3024	Lamotrigine Lamotrigine (BW-430C)是一种新型抗惊厥药剂，作用于人类血小板和大鼠脑突触体，抑制5-羟色胺(5-HT)吸收，IC50分别为240 μM和474 μM。	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1965	Primidone Primidone (NCI-C56360) 是一种嘧啶二酮类抗惊厥药。
S3064	Ambroxol HCl Ambroxol HCl是有效的神经性钠离子通道抑制剂，抑制抗TTX的钠离子电流，相位性阻滞，IC50为22.5 μM，抑制对TTX敏感的钠离子电流，IC50为100 μM。Phase 3。
S2041	Dyclonine HCl Dyclonine HCl是Dyclonine的盐酸盐形式，是一种口服麻醉剂。Dyclonine可逆地与神经元细胞膜上活化的钠离子通道结合，减少神经元膜对钠离子的通透性。
S4229	Oxybuprocaine HCl Oxybuprocaine HCl是一种局部麻醉剂，尤其在眼科与耳鼻咽喉科使用。其与钠离子通道结合，可逆地稳定神经元细胞膜，减少其对钠离子的通透性。
S3155	Mepivacaine HCl Mepivacaine 是一种叔胺，用作局部麻醉剂。
S2500	Propafenone HCl Propafenone HCl是一种典型的抗心律失常药物，用于治疗与心跳加速相关的疾病，如心房和心室心律失常。
S9142	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S4023	Procaine HCl Procaine (Novocaine) 是一种钠离子通道的，NMDA受体以及乙酰胆碱受体抑制剂， IC50分别为60 μM， 0.296 mM何45.5 μM，也是一种，5-HT3抑制剂，K_D为1.7 μM。	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
S1619	Prilocaine Prilocaine (NSC 40027) 是一种氨基酰胺类的局部麻醉剂。它作用于神经元细胞膜上的钠离子通道，限制癫痫发作的扩散。
S5556	(-)-Sparteine Sulfate Sparteine Sulfate, a quinolizidine alkaloid, is the sulfate form of sparteini, which is a sodium channel blocker used as an oxytocic and an anti-arrhythmia agent.
S5274	GS967 GS967 (GS458967) is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S4038	Dibucaine HCl Dibucaine HCl (Cinchocaine) 是一种局部麻醉剂。
S5490	Disopyramide Disopyramide is a class IA antiarrhythmic drug which acts via blockade of sodium channels depressing phase 0 of the action potential. Disopyramide possesses significant negative inotropic, anticholinergic effects and enhances AV nodal conduction.
S1391	Oxcarbazepine Oxcarbazepine (GP47680) 是一种抗惊厥和稳定情绪的药物。抑制[3H]BTX与sodium channels结合， IC50位160 μM，也抑制²²Na⁺汇入大鼠脑i突触体， IC50约为100 μM。
S4657	Eslicarbazepine Acetate Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom) 是一种抗癫痫药物。
S4058	Ropivacaine HCl Ropivacaine HCl (LEA-103) 是一种麻醉剂，通过可逆地抑制钠离子流入来阻断神经纤维上冲动的传导。	Cancer Discov, 2020, CD-20-0160
S4180	Nefopam HCl Nefopam HCl是一种中枢作用剂，但是是非阿片类的镇痛药，抑制电压门控钠通道，及抑制5-羟色胺，多巴胺和去甲肾上腺素的再吸收。
S4061	Levobupivacaine HCl Levobupivacaine HCl ((S)-(-)-Bupivacaine)，丁哌卡因的纯净S(-)-对映体,是一种可逆神经元的sodium channel抑制剂，用作长效局部麻醉剂。
S5814	cariporide Cariporide是有效的选择性NHE1抑制剂，在CHO-K1细胞中对hNHE1的IC50值为30 nM。	Int J Med Sci, 2020, 17(11):1652-1664
S4080	Triamterene Triamterene (SKF8542) 以电压依赖方式阻断上皮细胞钠离子通道(ENaC)，IC50值为4.5 μM.	Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S8615	Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂，对PDK2和PDK4的IC50值分别为183和80 μM；可抑制 Na⁺-K⁺-2Cl^- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成，引起癌细胞凋亡，并抑制肿瘤生长。	Cell Death Dis, 2020, 11(11):991
S5710	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S2318	Lappaconitine Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
S4200	Tolperisone HCl Tolperisone HCl是一种离子通道抑制剂和中枢性肌肉松弛剂。
S4210	Benzocaine Benzocaine 是对氨基苯甲酸乙酯 (PABA), 是一种局部麻醉剂，用作外用止痛药或常用于止咳。
S4669	Benzocaine hydrochloride Benzocaine hydrochloride (Ethyl 4-aminobenzoate, Ethyl p-aminobenzoate)是一种表面麻醉剂，通过阻止沿着神经纤维及在神经末梢的脉冲传播发挥作用。
S4668	Procaine Procaine (Novocaine, Vitamin H3, Duracaine, Spinocaine) 是苯甲酸类化合物，具有局部麻醉和抗心律失常的活性。Procaine结合并抑制电压依赖性钠离子通道，因而抑制脉冲起始和传导所需的离子通量。
S4225	Mexiletine HCl Mexiletine HCl (KO1173)属于IB类抗心律失常药，抑制钠离子通道，降低内流钠电流。	Biogerontology, 2016, 17(5-6):907-920
S4235	Phenazopyridine HCl Phenazopyridine HCl是一种局部镇痛剂，已被用于治疗泌尿系统疾病。它是sodium channel protein type 1 subunit alpha的抑制剂。	bioRxiv, 2020, 2020/9/20.4.7.30734
S3751	Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine)可抑制电压依赖性钠离子通道，同时也具有抗毒蕈碱和抗疟疾活性。	J Pharmacol Toxicol Methods, 2020, 106895
S3907	Bulleyaconi cine A Bulleyaconi cine A (Bulleyaconitine A, BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
S4284	Chloroprocaine HCl Chloroprocaine HCl 是手术治疗中的局部麻醉剂。
S5749	Chlorpromazine Chlorpromazine (CPZ) 是一种低效的典型抗精神病药，用于治疗精神病如精神分裂症。Chlorpromazine (CPZ) 在体外可抑制 5-HT(2A) receptor 和 dopamine D2。Chlorpromazine (CPZ) 还可抑制 sodium channel，并阻断HERG potassium channels，对应的IC50值为21.6 μM。	Biomaterials, 2020, 232:119701 Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734
S2110	Vinpocetine Vinpocetine (RGH-4405)选择性抑制电压敏感型钠离子通道，用于治疗中风，血管性痴呆和阿尔茨海默症。	An Acad Bras Cienc, 2020, 92(4):e20200241
S2118	Ibutilide Fumarate Ibutilide Fumarate (U-70226E)是第三类抗心律失常药物，主要用于急性新梗阻的心房颤动(房颤)/心房扑动(房扑)，适用于近期发作的房颤或房扑逆转成窦性心律，向内钠电流感应缓慢，这会延长心肌细胞的动作电位和不应期。	Gynecol Oncol, 2018, 151(3):525-532
S4294	Procainamide HCl Procainamide HCl是一种sodium channel的阻断剂，也是DNA甲基转移酶抑制剂，用于心律失常的治疗。
S3250^New	Veratrine Veratridine 是一种在百合科植物中发现的甾体生物碱，是 voltage-gated sodium channel 活化剂。Veratridine 会在大鼠中诱发类似焦虑的行为。
S3911	Veratramine Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
S1828	Proparacaine HCl Proparacaine HCl是电压门控的钠离子通道的拮抗剂，ED50是3.4 mM。

目录号	产品描述	文献引用	实验数据
S1614	Riluzole Riluzole (RP-54274, PK 26124) 是谷氨酸盐释放抑制剂，具有神经保护、抗癫痫、抗焦虑以及麻醉作用。	Cancer Res,2019, 79(8):1799-1809 Neuropharmacology,2019, 150:175-183 J Cell Biochem,2019, 10.1002/jcb.29533	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
S2454	Bupivacaine HCl Bupivacaine HCl 可以与钠离子通道的胞内部分结合从而阻断进入神经细胞的钠离子流，用于治疗心律不齐。	Int J Mol Sci,2019, 20(17) J Steroid Biochem Mol Biol,2017, 172:89-97 Breast Cancer Res Treat,2015, 150(3):535-45
S1811	Amiloride HCl Amiloride是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。	Signal Transduct Target Ther,2020, 5(1):214 PLoS Genet,2020, 16(10):e1009100 Drug Discov Ther,2020, 14(5):256-258
S1256	Rufinamide Rufinamide (CGP 33101)是一种电压门控式的sodium channel阻断剂，用作抗惊厥的药物。
S1603	Furosemide Furosemide 是一种有效的NKCC2抑制剂，用于治疗充血性心脏衰竭和水肿。	Sci Rep,2018, 8(1):9302 Biomed Pharmacother,2018, 101:145-154 Vascul Pharmacol,2017, 99:74-82
S6920^New	SEA0400 SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂，可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收，对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERK 和 p38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。
S4339^New	Meticrane Meticrane 是一种利尿剂，可抑制远曲小管中 reabsorption of sodium and chloride ions 的重吸收。Meticrane 可用于治疗原发性高血压。
S0016^New	SN-6 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3，对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
S1445	Zonisamide Zonisamide (CI-912)是FDA批准的抗癫痫药物，阻断电压依赖性钠（+）通道和T型钙离子通道。
S2524	Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin)是一种失活的电压门控钠离子通道稳定剂。
S1693	Carbamazepine Carbamazepine (Carbatrol, NSC 169864) 是一种钠离子通道抑制剂，作用于大鼠脑突触体时， IC50为131 μM。	PLoS One,2019, 14(2):e0211644 DNA Cell Biol,2019, 10.1089/dna.2018.4553
S2785	A-803467 A-803467是一种选择性Na_V1.8 channel抑制剂，IC50为8 nM，抑制抗河豚毒的电流，比作用于人类Na_V1.2， Na_V1.3， Na_V1.5和Na_V1.7选择性高100倍以上。
S2560	Amiloride HCl dihydrate Amiloride HCl dihydrate是一种有效的上皮细胞钠离子通道抑制剂。	PLoS Genet,2020, 16(10):e1009100 Sci Rep,2017, 7(1):5586 Peptides,2015, 73:67-76
S1287	Bumetanide Bumetanide是一种氨磺酰基类的袢利尿剂，用于治疗心脏衰竭。	Cell Mol Gastroenterol Hepatol,2019, 10.1016/j
S2525	Phenytoin Phenytoin (Diphenylhydantoin) 是一种失活的电压门控钠离子通道稳定剂。
S2874	Camostat Mesilate Camostat (FOY-305)是胰蛋白酶样的蛋白酶抑制剂，抑制上皮细胞钠离子通道(ENaC)功能，IC50为50 nM, 对Trypsin, Prostasin 和 Matriptase作用效果稍弱。	EMBO J,2020, e2020106057 Sci Immunol,2020, 13;5(47):eabc3582 bioRxiv,2020, 2020.11.04.364315
S2114	Dronedarone HCl Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。	Cell Syst,2019, 8(2):97-108 Nat Commun,2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
S3024	Lamotrigine Lamotrigine (BW-430C)是一种新型抗惊厥药剂，作用于人类血小板和大鼠脑突触体，抑制5-羟色胺(5-HT)吸收，IC50分别为240 μM和474 μM。	Cancer Cell Int,2020, 19;20:58 Hum Cell,2020, 10.1007/s13577-020-00425-8 Hum Cell,2020, 10.1007/s13577-020-00420-z
S1965	Primidone Primidone (NCI-C56360) 是一种嘧啶二酮类抗惊厥药。
S3064	Ambroxol HCl Ambroxol HCl是有效的神经性钠离子通道抑制剂，抑制抗TTX的钠离子电流，相位性阻滞，IC50为22.5 μM，抑制对TTX敏感的钠离子电流，IC50为100 μM。Phase 3。
S2041	Dyclonine HCl Dyclonine HCl是Dyclonine的盐酸盐形式，是一种口服麻醉剂。Dyclonine可逆地与神经元细胞膜上活化的钠离子通道结合，减少神经元膜对钠离子的通透性。
S4229	Oxybuprocaine HCl Oxybuprocaine HCl是一种局部麻醉剂，尤其在眼科与耳鼻咽喉科使用。其与钠离子通道结合，可逆地稳定神经元细胞膜，减少其对钠离子的通透性。
S3155	Mepivacaine HCl Mepivacaine 是一种叔胺，用作局部麻醉剂。
S2500	Propafenone HCl Propafenone HCl是一种典型的抗心律失常药物，用于治疗与心跳加速相关的疾病，如心房和心室心律失常。
S9142	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S4023	Procaine HCl Procaine (Novocaine) 是一种钠离子通道的，NMDA受体以及乙酰胆碱受体抑制剂， IC50分别为60 μM， 0.296 mM何45.5 μM，也是一种，5-HT3抑制剂，K_D为1.7 μM。	Biomol Ther (Seoul),2016, 24(5):489-94 Biomol Ther (Seoul),2016, 24(5):489-94	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
S1619	Prilocaine Prilocaine (NSC 40027) 是一种氨基酰胺类的局部麻醉剂。它作用于神经元细胞膜上的钠离子通道，限制癫痫发作的扩散。
S5556	(-)-Sparteine Sulfate Sparteine Sulfate, a quinolizidine alkaloid, is the sulfate form of sparteini, which is a sodium channel blocker used as an oxytocic and an anti-arrhythmia agent.
S5274	GS967 GS967 (GS458967) is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S4038	Dibucaine HCl Dibucaine HCl (Cinchocaine) 是一种局部麻醉剂。
S5490	Disopyramide Disopyramide is a class IA antiarrhythmic drug which acts via blockade of sodium channels depressing phase 0 of the action potential. Disopyramide possesses significant negative inotropic, anticholinergic effects and enhances AV nodal conduction.
S1391	Oxcarbazepine Oxcarbazepine (GP47680) 是一种抗惊厥和稳定情绪的药物。抑制[3H]BTX与sodium channels结合， IC50位160 μM，也抑制²²Na⁺汇入大鼠脑i突触体， IC50约为100 μM。
S4657	Eslicarbazepine Acetate Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom) 是一种抗癫痫药物。
S4058	Ropivacaine HCl Ropivacaine HCl (LEA-103) 是一种麻醉剂，通过可逆地抑制钠离子流入来阻断神经纤维上冲动的传导。	Cancer Discov,2020, CD-20-0160
S4180	Nefopam HCl Nefopam HCl是一种中枢作用剂，但是是非阿片类的镇痛药，抑制电压门控钠通道，及抑制5-羟色胺，多巴胺和去甲肾上腺素的再吸收。
S4061	Levobupivacaine HCl Levobupivacaine HCl ((S)-(-)-Bupivacaine)，丁哌卡因的纯净S(-)-对映体,是一种可逆神经元的sodium channel抑制剂，用作长效局部麻醉剂。
S5814	cariporide Cariporide是有效的选择性NHE1抑制剂，在CHO-K1细胞中对hNHE1的IC50值为30 nM。	Int J Med Sci,2020, 17(11):1652-1664
S4080	Triamterene Triamterene (SKF8542) 以电压依赖方式阻断上皮细胞钠离子通道(ENaC)，IC50值为4.5 μM.	Cell Chem Biol,2020, 24 pii: S2451-9456(20)30080-5
S8615	Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂，对PDK2和PDK4的IC50值分别为183和80 μM；可抑制 Na⁺-K⁺-2Cl^- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成，引起癌细胞凋亡，并抑制肿瘤生长。	Cell Death Dis,2020, 11(11):991
S5710	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S2318	Lappaconitine Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
S4200	Tolperisone HCl Tolperisone HCl是一种离子通道抑制剂和中枢性肌肉松弛剂。
S4210	Benzocaine Benzocaine 是对氨基苯甲酸乙酯 (PABA), 是一种局部麻醉剂，用作外用止痛药或常用于止咳。
S4669	Benzocaine hydrochloride Benzocaine hydrochloride (Ethyl 4-aminobenzoate, Ethyl p-aminobenzoate)是一种表面麻醉剂，通过阻止沿着神经纤维及在神经末梢的脉冲传播发挥作用。
S4668	Procaine Procaine (Novocaine, Vitamin H3, Duracaine, Spinocaine) 是苯甲酸类化合物，具有局部麻醉和抗心律失常的活性。Procaine结合并抑制电压依赖性钠离子通道，因而抑制脉冲起始和传导所需的离子通量。
S4225	Mexiletine HCl Mexiletine HCl (KO1173)属于IB类抗心律失常药，抑制钠离子通道，降低内流钠电流。	Biogerontology,2016, 17(5-6):907-920
S4235	Phenazopyridine HCl Phenazopyridine HCl是一种局部镇痛剂，已被用于治疗泌尿系统疾病。它是sodium channel protein type 1 subunit alpha的抑制剂。	bioRxiv,2020, 2020/9/20.4.7.30734
S3751	Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine)可抑制电压依赖性钠离子通道，同时也具有抗毒蕈碱和抗疟疾活性。	J Pharmacol Toxicol Methods,2020, 106895
S3907	Bulleyaconi cine A Bulleyaconi cine A (Bulleyaconitine A, BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
S4284	Chloroprocaine HCl Chloroprocaine HCl 是手术治疗中的局部麻醉剂。
S5749	Chlorpromazine Chlorpromazine (CPZ) 是一种低效的典型抗精神病药，用于治疗精神病如精神分裂症。Chlorpromazine (CPZ) 在体外可抑制 5-HT(2A) receptor 和 dopamine D2。Chlorpromazine (CPZ) 还可抑制 sodium channel，并阻断HERG potassium channels，对应的IC50值为21.6 μM。	Biomaterials,2020, 232:119701 Drug Metab Dispos,2020, 48(8):613-621 bioRxiv,2020, 2020/9/20.4.7.30734
S2110	Vinpocetine Vinpocetine (RGH-4405)选择性抑制电压敏感型钠离子通道，用于治疗中风，血管性痴呆和阿尔茨海默症。	An Acad Bras Cienc,2020, 92(4):e20200241
S2118	Ibutilide Fumarate Ibutilide Fumarate (U-70226E)是第三类抗心律失常药物，主要用于急性新梗阻的心房颤动(房颤)/心房扑动(房扑)，适用于近期发作的房颤或房扑逆转成窦性心律，向内钠电流感应缓慢，这会延长心肌细胞的动作电位和不应期。	Gynecol Oncol,2018, 151(3):525-532
S4294	Procainamide HCl Procainamide HCl是一种sodium channel的阻断剂，也是DNA甲基转移酶抑制剂，用于心律失常的治疗。

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S3250^New	Veratrine Veratridine 是一种在百合科植物中发现的甾体生物碱，是 voltage-gated sodium channel 活化剂。Veratridine 会在大鼠中诱发类似焦虑的行为。

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S3250^New

Veratrine

Veratridine 是一种在百合科植物中发现的甾体生物碱，是 voltage-gated sodium channel 活化剂。Veratridine 会在大鼠中诱发类似焦虑的行为。

目录号	产品描述	文献引用	实验数据
S3911	Veratramine Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
S1828	Proparacaine HCl Proparacaine HCl是电压门控的钠离子通道的拮抗剂，ED50是3.4 mM。

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S3911

Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.

S1828

Proparacaine HCl

Proparacaine HCl是电压门控的钠离子通道的拮抗剂，ED50是3.4 mM。

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