Target Information
| Target General Information | Top | |||||
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| Target ID |
T39716
(Former ID: TTDS00402)
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| Target Name |
Voltage-gated sodium channel alpha Nav1.5 (SCN5A)
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| Synonyms |
Voltage-gated sodium channel subunit alpha Nav1.5; Sodium channel protein type V subunit alpha; Sodium channel protein type 5 subunit alpha; Sodium channel protein cardiac muscle subunit alpha; HH1
Click to Show/Hide
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| Gene Name |
SCN5A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 8 Target-related Diseases | + | ||||
| 1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
| 2 | Cardiac arrhythmia [ICD-11: BC9Z] | |||||
| 3 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 4 | Cough [ICD-11: MD12] | |||||
| 5 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
| 6 | Migraine [ICD-11: 8A80] | |||||
| 7 | Pain [ICD-11: MG30-MG3Z] | |||||
| 8 | Ventricular tachyarrhythmia [ICD-11: BC71] | |||||
| Function |
Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels. This protein mediates the voltage-dependent sodium ion permeability of excitable membranes.
Click to Show/Hide
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| BioChemical Class |
Voltage-gated ion channel
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| UniProt ID | ||||||
| Sequence |
MANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQA
SKKLPDLYGNPPQELIGEPLEDLDPFYSTQKTFIVLNKGKTIFRFSATNALYVLSPFHPI RRAAVKILVHSLFNMLIMCTILTNCVFMAQHDPPPWTKYVEYTFTAIYTFESLVKILARG FCLHAFTFLRDPWNWLDFSVIIMAYTTEFVDLGNVSALRTFRVLRALKTISVISGLKTIV GALIQSVKKLADVMVLTVFCLSVFALIGLQLFMGNLRHKCVRNFTALNGTNGSVEADGLV WESLDLYLSDPENYLLKNGTSDVLLCGNSSDAGTCPEGYRCLKAGENPDHGYTSFDSFAW AFLALFRLMTQDCWERLYQQTLRSAGKIYMIFFMLVIFLGSFYLVNLILAVVAMAYEEQN QATIAETEEKEKRFQEAMEMLKKEHEALTIRGVDTVSRSSLEMSPLAPVNSHERRSKRRK RMSSGTEECGEDRLPKSDSEDGPRAMNHLSLTRGLSRTSMKPRSSRGSIFTFRRRDLGSE ADFADDENSTAGESESHHTSLLVPWPLRRTSAQGQPSPGTSAPGHALHGKKNSTVDCNGV VSLLGAGDPEATSPGSHLLRPVMLEHPPDTTTPSEEPGGPQMLTSQAPCVDGFEEPGARQ RALSAVSVLTSALEELEESRHKCPPCWNRLAQRYLIWECCPLWMSIKQGVKLVVMDPFTD LTITMCIVLNTLFMALEHYNMTSEFEEMLQVGNLVFTGIFTAEMTFKIIALDPYYYFQQG WNIFDSIIVILSLMELGLSRMSNLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALG NLTLVLAIIVFIFAVVGMQLFGKNYSELRDSDSGLLPRWHMMDFFHAFLIIFRILCGEWI ETMWDCMEVSGQSLCLLVFLLVMVIGNLVVLNLFLALLLSSFSADNLTAPDEDREMNNLQ LALARIQRGLRFVKRTTWDFCCGLLRQRPQKPAALAAQGQLPSCIATPYSPPPPETEKVP PTRKETRFEEGEQPGQGTPGDPEPVCVPIAVAESDTDDQEEDEENSLGTEEESSKQQESQ PVSGGPEAPPDSRTWSQVSATASSEAEASASQADWRQQWKAEPQAPGCGETPEDSCSEGS TADMTNTAELLEQIPDLGQDVKDPEDCFTEGCVRRCPCCAVDTTQAPGKVWWRLRKTCYH IVEHSWFETFIIFMILLSSGALAFEDIYLEERKTIKVLLEYADKMFTYVFVLEMLLKWVA YGFKKYFTNAWCWLDFLIVDVSLVSLVANTLGFAEMGPIKSLRTLRALRPLRALSRFEGM RVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFGRCINQTEGDLPLNYTIVNN KSQCESLNLTGELYWTKVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRGYEEQPQW EYNLYMYIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKK LGSKKPQKPIPRPLNKYQGFIFDIVTKQAFDVTIMFLICLNMVTMMVETDDQSPEKINIL AKINLLFVAIFTGECIVKLAALRHYYFTNSWNIFDFVVVILSIVGTVLSDIIQKYFFSPT LFRVIRLARIGRILRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMANFA YVKWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPTLPNSNGSRG DCGSPAVGILFFTTYIIISFLIVVNMYIAIILENFSVATEESTEPLSEDDFDMFYEIWEK FDPEATQFIEYSVLSDFADALSEPLRIAKPNQISLINMDLPMVSGDRIHCMDILFAFTKR VLGESGEMDALKIQMEEKFMAANPSKISYEPITTTLRRKHEEVSAMVIQRAFRRHLLQRS LKHASFLFRQQAGSGLSEEDAPEREGLIAYVMSENFSRPLGPPSSSSISSTSFPPSYDSV TRATSDNLQVRGSDYSHSEDLADFPPSPDRDRESIV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A04830 | |||||
| HIT2.0 ID | T77X36 | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 14 Approved Drugs | + | ||||
| 1 | Benzonatate | Drug Info | Approved | Cough | [2], [3] | |
| 2 | Dibucaine | Drug Info | Approved | Anaesthesia | [4], [5], [6] | |
| 3 | Disopyramide | Drug Info | Approved | Ventricular arrhythmias | [7], [8] | |
| 4 | Dyclonine | Drug Info | Approved | Pain | [6], [9], [10] | |
| 5 | Ethotoin | Drug Info | Approved | Complex partial seizure | [11], [12] | |
| 6 | Fosphenytoin | Drug Info | Approved | Epilepsy | [6] | |
| 7 | Hexylcaine | Drug Info | Approved | Anaesthesia | [6] | |
| 8 | Indecainide | Drug Info | Approved | Dysrhythmias | [13] | |
| 9 | LOMERIZINE | Drug Info | Approved | Migraine | [6], [14] | |
| 10 | Mephenytoin | Drug Info | Approved | Epilepsy | [15], [16] | |
| 11 | Mexiletine | Drug Info | Approved | Ventricular tachycardia | [6] | |
| 12 | Moricizine | Drug Info | Approved | Arrhythmia | [6] | |
| 13 | Prilocaine | Drug Info | Approved | Pain | [6], [17], [18] | |
| 14 | Tetrodotoxin | Drug Info | Approved | Bacterial infection | [19], [20] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | F-15845 | Drug Info | Phase 1 | Angina pectoris | [21] | |
| Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
| 1 | Encainide | Drug Info | Withdrawn from market | Heart arrhythmia | [22], [6] | |
| 2 | LUBELUZOLE | Drug Info | Discontinued in Preregistration | Neurological disorder | [23] | |
| 3 | Acecainide | Drug Info | Discontinued in Phase 3 | Solid tumour/cancer | [24] | |
| 4 | SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disorder | [25] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Blocker | [+] 16 Blocker drugs | + | ||||
| 1 | Benzonatate | Drug Info | [26] | |||
| 2 | Dibucaine | Drug Info | [20] | |||
| 3 | Disopyramide | Drug Info | [27] | |||
| 4 | Dyclonine | Drug Info | [28] | |||
| 5 | Ethotoin | Drug Info | [26] | |||
| 6 | Fosphenytoin | Drug Info | [29] | |||
| 7 | Hexylcaine | Drug Info | [26] | |||
| 8 | Indecainide | Drug Info | [1] | |||
| 9 | Mephenytoin | Drug Info | [29] | |||
| 10 | Mexiletine | Drug Info | [27] | |||
| 11 | Moricizine | Drug Info | [31] | |||
| 12 | Prilocaine | Drug Info | [28] | |||
| 13 | Tetrodotoxin | Drug Info | [20] | |||
| 14 | Dihydrobenzoxazine and tetrahydroquinoxaline sulfonamide derivative 1 | Drug Info | [34] | |||
| 15 | Encainide | Drug Info | [31] | |||
| 16 | Acecainide | Drug Info | [28] | |||
| Inhibitor | [+] 12 Inhibitor drugs | + | ||||
| 1 | LOMERIZINE | Drug Info | [30] | |||
| 2 | F-15845 | Drug Info | [32], [33] | |||
| 3 | Aryl carboxamide derivative 1 | Drug Info | [34] | |||
| 4 | Aryl carboxamide derivative 2 | Drug Info | [34] | |||
| 5 | Aryl carboxamide derivative 3 | Drug Info | [34] | |||
| 6 | LUBELUZOLE | Drug Info | [30] | |||
| 7 | SIPATRIGINE | Drug Info | [30] | |||
| 8 | PD-85639 | Drug Info | [30] | |||
| 9 | 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | [35] | |||
| 10 | KC-12291 | Drug Info | [38] | |||
| 11 | N-(4-Methyl-benzoyl)-N'-phenethyl-guanidine | Drug Info | [39] | |||
| 12 | N-Butyl-N'-(4-methyl-benzoyl)-guanidine | Drug Info | [39] | |||
| Activator | [+] 3 Activator drugs | + | ||||
| 1 | aconitine | Drug Info | [36] | |||
| 2 | batrachotoxin | Drug Info | [37] | |||
| 3 | veratridine | Drug Info | [40] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Quinidine | Ligand Info | |||||
| Structure Description | voltage-gated sodium channel Nav1.5 with quinidine | PDB:6LQA | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | No | [41] |
| PDB Sequence |
PIRRAAVKIL
128 VHSLFNMLIM138 CTILTNCVFM148 AQHDPPPWTK158 YVEYTFTAIY168 TFESLVKILA 178 RGFCLHAFTF188 LRDPWNWLDF198 SVIIMAYTTE208 FVDLGNVSAL218 RTFRVLRALK 228 TISVISGLKT238 IVGALIQSVK248 KLADVMVLTV258 FCLSVFALIG268 LQLFMGNLRH 278 KCVRNFTALN288 GTNGSVEADG298 LVWESLDLYL308 SDPENYLLKN318 GTSDVLLCGN 328 SSDAGTCPEG338 YRCLKAGENP348 DHGYTSFDSF358 AWAFLALFRL368 MTQDCWERLY 378 QQTLRSAGKI388 YMIFFMLVIF398 LGSFYLVNLI408 LAVVAMAYEE418 QNQATIAETE 428 ECCPLWMSIK707 QGVKLVVMDP717 FTDLTITMCI727 VLNTLFMALE737 HYNMTSEFEE 747 MLQVGNLVFT757 GIFTAEMTFK767 IIALDPYYYF777 QQGWNIFDSI787 IVILSLMELG 797 LSRMSNLSVL807 RSFRLLRVFK817 LAKSWPTLNT827 LIKIIGNSVG837 ALGNLTLVLA 847 IIVFIFAVVG857 MQLFGKNYSE867 LRDSDSGLLP877 RWHMMDFFHA887 FLIIFRILCG 897 EWIETMWDCM907 EVSGQSLCLL917 VFLLVMVIGN927 LVVLNLFLAL937 LLSSFSAGKV 1190 WWRLRKTCYH1200 IVEHSWFETF1210 IIFMILLSSG1220 ALAFEDIYLE1230 ERKTIKVLLE 1240 YADKMFTYVF1250 VLEMLLKWVA1260 YGFKKYFTNA1270 WCWLDFLIVD1280 VSLVSLVANT 1290 LGFAEMGPIK1300 SLRTLRALRP1310 LRALSRFEGM1320 RVVVNALVGA1330 IPSIMNVLLV 1340 CLIFWLIFSI1350 MGVNLFAGKF1360 GRCINQTEGD1370 LPLNYTIVNN1380 KSQCESLNLT 1390 GELYWTKVKV1400 NFDNVGAGYL1410 ALLQVATFKG1420 WMDIMYAAVD1430 SRGYEEQPQW 1440 EYNLYMYIYF1450 VIFIIFGSFF1460 TLNLFIGVII1470 DNFNQQKKKL1480 GGQDIFMTEE 1490 QKKYYNAMKK1500 LGSKKPQKPI1510 PRPLNKYQGF1520 IFDIVTKQAF1530 DVTIMFLICL 1540 NMVTMMVETD1550 DQSPEKINIL1560 AKINLLFVAI1570 FTGECIVKLA1580 ALRHYYFTNS 1590 WNIFDFVVVI1600 LSIVGTVLSD1610 IIQKYFFSPT1620 LFRVIRLARI1630 GRILRLIRGA 1640 KGIRTLLFAL1650 MMSLPALFNI1660 GLLLFLVMFI1670 YSIFGMANFA1680 YVKWEAGIDD 1690 MFNFQTFANS1700 MLCLFQITTS1710 AGWDGLLSPI1720 LNTGPPYCDP1730 TLPNSNGSRG 1740 DCGSPAVGIL1750 FFTTYIIISF1760 LIVVNMYIAI1770 ILENFSVATE1780 E |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| Polycystin family receptor for egg jelly (PKDREJ) | 20.513 (56/273) | 8.79E-05 | |
| Sodium/hydrogen exchanger 11 (SLC9C2) | 27.273 (36/132) | 1.88E-04 |
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Adrenergic signaling in cardiomyocytes | hsa04261 | Affiliated Target |
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| Class: Organismal Systems => Circulatory system | Pathway Hierarchy | ||
| Degree | 12 | Degree centrality | 1.29E-03 | Betweenness centrality | 1.80E-03 |
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| Closeness centrality | 2.05E-01 | Radiality | 1.36E+01 | Clustering coefficient | 9.09E-02 |
| Neighborhood connectivity | 1.01E+01 | Topological coefficient | 1.01E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | Adrenergic signaling in cardiomyocytes | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Muscle/Heart Contraction | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Interaction between L1 and Ankyrins | |||||
| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | Cardiac Progenitor Differentiation | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Electrophysiological studies of indecainide hydrochloride, a new antiarrhythmic agent, in canine cardiac tissues. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):614-21. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7611). | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040587. | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7159). | |||||
| REF 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006203. | |||||
| REF 6 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7167). | |||||
| REF 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070101. | |||||
| REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7173). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009925. | |||||
| REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7183). | |||||
| REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010841. | |||||
| REF 13 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019693. | |||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002033) | |||||
| REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7223). | |||||
| REF 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006008. | |||||
| REF 17 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7276). | |||||
| REF 18 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076290. | |||||
| REF 19 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2616). | |||||
| REF 20 | Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81. | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023448) | |||||
| REF 22 | New antiarrhythmic drugs: tocainide, mexiletine, flecainide, encainide, and amiodarone. Mayo Clin Proc. 1987 Nov;62(11):1033-50. | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005388) | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000315) | |||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904) | |||||
| REF 26 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 27 | Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9. | |||||
| REF 28 | Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12. | |||||
| REF 29 | Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68. | |||||
| REF 30 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37. | |||||
| REF 31 | From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33. | |||||
| REF 32 | Selective inhibition of persistent sodium current by F 15845 prevents ischaemia-induced arrhythmias. Br J Pharmacol. 2010 Sep;161(1):79-91. | |||||
| REF 33 | A rare loss-of-function SCN5A variant is associated with lidocaine-induced ventricular fibrillation. Pharmacogenomics J. 2014 Aug;14(4):372-5. | |||||
| REF 34 | Sodium channel blockers: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015 Mar;25(3):279-90. | |||||
| REF 35 | Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. | |||||
| REF 36 | Properties of aconitine-modified sodium channels in single cells of mouse ventricular myocardium. Gen Physiol Biophys. 1986 Oct;5(5):473-84. | |||||
| REF 37 | Binding of [3H]batrachotoxinin A benzoate to specific sites on rat cardiac sodium channels. Mol Pharmacol. 1986 Dec;30(6):617-23. | |||||
| REF 38 | Sodium late current blockers in ischemia reperfusion: is the bullet magic J Med Chem. 2008 Jul 10;51(13):3856-66. | |||||
| REF 39 | Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers. Bioorg Med Chem Lett. 2001 Dec 17;11(24):3151-5. | |||||
| REF 40 | Sodium channel comodification with full activator reveals veratridine reaction dynamics. Mol Pharmacol. 1990 Feb;37(2):144-8. | |||||
| REF 41 | Structural Basis for Pore Blockade of the Human Cardiac Sodium Channel Na(v) 1.5 by the Antiarrhythmic Drug Quinidine*. Angew Chem Int Ed Engl. 2021 May 10;60(20):11474-11480. | |||||
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