Target Information

Target General Infomation
Target ID
T39716
Former ID
TTDS00402
Target Name
Sodium channel protein type 5 subunit alpha
Gene Name
SCN5A
Synonyms
HH1; Sodium channel protein cardiac muscle subunit alpha; Sodium channel protein type V subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.5; SCN5A
Target Type
Successful
Disease Angina pectoris [ICD9: 413; ICD10: I20]
Anesthesia [ICD9: 338; ICD10: R20.0]
Anesthesia; Hemorrhoids [ICD9:338; ICD10: R20.0, I84]
Arrhythmia [ICD9: 427; ICD10: I47-I49]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Complex partial seizures [ICD9: 345.4; ICD10: G40.2]
Cough [ICD9: 786.2; ICD10: R05]
Dysrhythmias [ICD9: 427; ICD10: I47-I49]
Epilepsy [ICD10: G40]
Epilepsy; Convulsion [ICD10: G40]
Heart arrhythmia [ICD10: I47-I49]
Local anaesthetic [ICD10: R20.0]
Migraine [ICD9: 346; ICD10: G43]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Ventricular arrhythmias [ICD9: 427.1; ICD10: I47.2]
Ventricular tachycardia; Symptomatic premature ventricular beats; Ventricular fibrillation [ICD10: I47.2]
BioChemical Class
Voltage-gated ion channel
Target Validation
T39716
UniProt ID
Q14524
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
Drugs and Mode of Action
Drug(s) Benzonatate Drug Info Approved Cough [538191], [542600]
Dibucaine Drug Info Approved Anesthesia; Hemorrhoids [538393], [542167], [551871]
Disopyramide Drug Info Approved Ventricular arrhythmias [538219], [542176]
Dyclonine Drug Info Approved Pain [538425], [542183], [551871]
Ethotoin Drug Info Approved Complex partial seizures [538439], [542194]
Fosphenytoin Drug Info Approved Epilepsy; Convulsion [551871]
Hexylcaine Drug Info Approved Local anaesthetic [551871]
Indecainide Drug Info Approved Dysrhythmias [538531]
LOMERIZINE Drug Info Approved Migraine [545070], [551871]
Mephenytoin Drug Info Approved Epilepsy [538388], [542238]
Mexiletine Drug Info Approved Ventricular tachycardia; Symptomatic premature ventricular beats; Ventricular fibrillation [551871]
Moricizine Drug Info Approved Arrhythmia [551871]
Prilocaine Drug Info Approved Pain [538314], [542296], [551871]
Tetrodotoxin Drug Info Approved Bacterial infections [535573], [539688]
F-15845 Drug Info Phase 1 Angina pectoris [548229]
Disopyramide Drug Info Withdrawn from market Urinary incontinence [542176], [551871]
Encainide Drug Info Withdrawn from market Heart arrhythmia [537733], [551871]
Hexylcaine Drug Info Withdrawn from market Anesthesia [538409], [542208]
Moricizine Drug Info Withdrawn from market Heart arrhythmia [538532], [542261], [551871]
LUBELUZOLE Drug Info Discontinued in Preregistration Neurological disease [545928]
SIPATRIGINE Drug Info Discontinued in Phase 2 Neurological disease [545614]
PD-85639 Drug Info Terminated Discovery agent [545294]
Inhibitor 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine Drug Info [529491]
F-15845 Drug Info [531108], [532635]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info [525961]
KC-12291 Drug Info [529518]
LOMERIZINE Drug Info [525961]
LUBELUZOLE Drug Info [525961]
N-(4-Methyl-benzoyl)-N'-phenethyl-guanidine Drug Info [526204]
N-Butyl-N'-(4-methyl-benzoyl)-guanidine Drug Info [526204]
PD-85639 Drug Info [525961]
SIPATRIGINE Drug Info [525961]
Blocker Acetylprocainamide Drug Info [538082]
Benzonatate Drug Info [536316]
Dibucaine Drug Info [535573]
Disopyramide Drug Info [535117]
Dyclonine Drug Info [538082]
Encainide Drug Info [537980]
Ethotoin Drug Info [536316]
Fosphenytoin Drug Info [537516]
Hexylcaine Drug Info [536316]
Indecainide Drug Info [537786]
Mephenytoin Drug Info [537516]
Mexiletine Drug Info [535117]
Moricizine Drug Info [537980]
Prilocaine Drug Info [538082]
Tetrodotoxin Drug Info [535573]
Activator aconitine Drug Info [532584]
batrachotoxin Drug Info [532575]
veratridine Drug Info [531463]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Adrenergic signaling in cardiomyocytes
PathWhiz Pathway Muscle/Heart Contraction
Reactome Interaction between L1 and Ankyrins
WikiPathways SIDS Susceptibility Pathways
Cardiac Progenitor Differentiation
References
Ref 535573Halothane 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 537733New antiarrhythmic drugs: tocainide, mexiletine, flecainide, encainide, and amiodarone. Mayo Clin Proc. 1987 Nov;62(11):1033-50.
Ref 538191FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040587.
Ref 538219FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070101.
Ref 538314FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076290.
Ref 538388FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006008.
Ref 538393FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006203.
Ref 538409FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008472.
Ref 538425FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009925.
Ref 538439FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010841.
Ref 538531FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019693.
Ref 538532FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019753.
Ref 539688(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 542167(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 542176(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 542183(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 542194(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 542208(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: 7196).
Ref 542238(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 542261(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: 7244).
Ref 542296(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 542600(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 545070Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002033)
Ref 545294Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002730)
Ref 545614Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904)
Ref 545928Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005388)
Ref 548229Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023448)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 526204Bioorg Med Chem Lett. 2001 Dec 17;11(24):3151-5.Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Ref 529491Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. Epub 2008 May 6.Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Ref 529518J Med Chem. 2008 Jul 10;51(13):3856-66. Epub 2008 Jun 5.Sodium late current blockers in ischemia reperfusion: is the bullet magic?.
Ref 531108Selective inhibition of persistent sodium current by F 15845 prevents ischaemia-induced arrhythmias. Br J Pharmacol. 2010 Sep;161(1):79-91.
Ref 531463Sodium channel comodification with full activator reveals veratridine reaction dynamics. Mol Pharmacol. 1990 Feb;37(2):144-8.
Ref 532575Binding of [3H]batrachotoxinin A benzoate to specific sites on rat cardiac sodium channels. Mol Pharmacol. 1986 Dec;30(6):617-23.
Ref 532584Properties of aconitine-modified sodium channels in single cells of mouse ventricular myocardium. Gen Physiol Biophys. 1986 Oct;5(5):473-84.
Ref 532635A rare loss-of-function SCN5A variant is associated with lidocaine-induced ventricular fibrillation. Pharmacogenomics J. 2014 Aug;14(4):372-5.
Ref 535117Effect 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 535573Halothane 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 536316How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 537516Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68. doi: 10.2165/00023210-200923070-00002.
Ref 537786Electrophysiological studies of indecainide hydrochloride, a new antiarrhythmic agent, in canine cardiac tissues. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):614-21.
Ref 537980From 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 538082Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12.

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