Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00402

Target Information
NameSodium channel protein type 5 subunit alpha    
Type of targetSuccessful target    
SynonymsHH1    
SCN5A    
Sodium channel protein cardiac muscle subunit alpha    
Sodium channel protein type V subunit alpha    
Voltage-gated sodium channel subunit alpha Nav1.5    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Cardiac dysrhythmias
[ICD9: 427   ICD10: I47-I49]
[2]
Epileptic seizures
[ICD9: 345.9, 780.3   ICD10: G40, P90, R56]
[3]
Pain
[ICD9: 338,780   ICD10: R52, G89]
[1]
Refractory partial epilepsy
[ICD9: 345   ICD10: G40]
[3]
Sustained ventricular tachycardia
[ICD9: 427, 427.1, 785.0   ICD10: I47-I49, I47.2, R00.0]
[2]
Drug(s)BenzonatateApprovedCough[4]
DibucaineApprovedAnesthetic[5]
DisopyramideApprovedVentricular arrhythmias[2]
DyclonineApprovedAnesthetic[6]
EncainideApprovedIrregular heartbeats[7]
EthotoinApprovedComplex partial seizures[4]
FlecainideApprovedTachyarrhythmias[2]
FosphenytoinApprovedSeizures[3]
HexylcaineApprovedAnesthetic[4]
IndecainideApprovedDysrhythmias[8]
MephenytoinApprovedEpilepsy[3]
MexiletineApprovedVentricular arrhythmias[2]
MoricizineApprovedIrregular heartbeats[7]
PrilocaineApprovedAnesthetic[6]
ProcainamideApprovedVentricular arrhythmias[9]
ProparacaineApprovedAnesthetic[6]
QuinidineApprovedVentricular arrhythmias[6]
TetrodotoxinApprovedBacterial infections[5]
TocainideApprovedVentricular arrhythmias[10]
BioChemical ClassVoltage-gated channel    
UniProt IDQ14524
PDB Structure2KBI.    
SequenceMANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQA 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
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-[5- (4-Chlorophenyl)-2-furoyl]piperazine[11]
Enecadin[12]
Indol-1-yl-propyl-pyridin-4-yl-amine (Besipirdine)[12]
KC-12291[13]
LOMERIZINE[12]
LUBELUZOLE[12]
N- (4-Methyl-benzoyl)-N'-phenethyl-guanidine[14]
N-Butyl-N'- (4-methyl-benzoyl)-guanidine[14]
PD-85639[12]
SIPATRIGINE[12]
BlockerAcetylprocainamide[6]
Benzonatate[4]
Dibucaine[5]
Disopyramide[2]
Dyclonine[6]
Encainide[7]
Ethotoin[4]
Flecainide[2]
Fosphenytoin[3]
Hexylcaine[4]
Indecainide[8]
Mephenytoin[3]
Mexiletine[2]
Moricizine[7]
Prilocaine[6]
Procainamide[9]
Proparacaine[6]
Quinidine[6]
Tetrodotoxin[5]
Tocainide[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Challenges in Analgesic Drug Development. Clin Pharmacol Ther. 2009 Aug 12. To Reference
Ref 2Effect 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. To Reference
Ref 3Lacosamide: 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. To Reference
Ref 4How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 5Halothane 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. To Reference
Ref 6Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12. To Reference
Ref 7From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33. To Reference
Ref 8Electrophysiological studies of indecainide hydrochloride, a new antiarrhythmic agent, in canine cardiac tissues. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):614-21. To Reference
Ref 9Isolated perfused and paced guinea pig heart to test for drug-induced changes of the QT interval. J Pharmacol Toxicol Methods. 2006 Nov-Dec;54(3):278-87. Epub 2006 Feb 28. To Reference
Ref 102D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers. Eur J Med Chem. 2009 Apr;44(4):1477-85. Epub 2008 Oct 14. To Reference
Ref 11Bioorg 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. To Reference
Ref 12J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. To Reference
Ref 13J Med Chem. 2008 Jul 10;51(13):3856-66. Epub 2008 Jun 5.Sodium late current blockers in ischemia reperfusion: is the bullet magic? To Reference
Ref 14Bioorg 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. To Reference



 

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