Target Information

Target General Infomation
Target ID
T29303
Former ID
TTDS00155
Target Name
Sodium channel
Gene Name
SCN1A
Synonyms
NAC1; SCN1; Sodium channel protein type I subunit alpha; Sodium channel protein, brain I subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.1; SCN1A
Target Type
Successful
Disease Angina pectoris [ICD9: 413; ICD10: I20]
Anesthesia [ICD9: 338; ICD10: R20.0]
Bipolar disorder [ICD9: 296.0, 296.1, 296.4, 296.5, 296.6, 296.7, 296.8, 300; ICD10: F31, F40-F42]
Cardiac failure [ICD10: I50]
Cough [ICD9: 786.2; ICD10: R05]
Cardiovascular disorder [ICD10: I00-I99]
Cerebral infarction [ICD10: I63]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
Cystic fibrosis [ICD9: 277; ICD10: E84]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Epilepsy [ICD10: G40]
Epilepsy; Focal; Seizure disorder [ICD9: 345, 345.4, 345.5, 345.9, 780.3; ICD10: G40, G40.2, P90, R56]
Gastric cancer [ICD9: 151; ICD10: C16]
Heart arrhythmia [ICD10: I47-I49]
Infections with sarcoptes scabiei [ICD9: 133; ICD10: B86]
Ischemia [ICD9: 459.89; ICD10: I99.8]
Local or regional analgesia and anesthesia [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]
Nerve injury [ICD10: T14.4]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Oxytocic [ICD10: O00-O99]
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Parkinson's disease [ICD9: 332; ICD10: G20]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Peripheral neuropathy [ICD10: G64]
Seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Seizures occurring during or following neurosurgery [ICD10: G40]
Seizures associated with lennox-Gastaut syndrome [ICD10: R56.9]
Spasm [ICD9: 728.85; ICD10: R25.2]
Schizophrenia [ICD9: 295; ICD10: F20]
Type 1 diabetes [ICD9: 250; ICD10: E10]
Urea cycle disorders [ICD9: 270.6; ICD10: E72.2]
Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes. 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.
BioChemical Class
Sodium channel
Target Validation
T29303
UniProt ID
P35498
Sequence
MEQTVLVPPGPDSFNFFTRESLAAIERRIAEEKAKNPKPDKKDDDENGPKPNSDLEAGKN
LPFIYGDIPPEMVSEPLEDLDPYYINKKTFIVLNKGKAIFRFSATSALYILTPFNPLRKI
AIKILVHSLFSMLIMCTILTNCVFMTMSNPPDWTKNVEYTFTGIYTFESLIKIIARGFCL
EDFTFLRDPWNWLDFTVITFAYVTEFVDLGNVSALRTFRVLRALKTISVIPGLKTIVGAL
IQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCIQWPPTNASLEEHSIEKNITVNY
NGTLINETVFEFDWKSYIQDSRYHYFLEGFLDALLCGNSSDAGQCPEGYMCVKAGRNPNY
GYTSFDTFSWAFLSLFRLMTQDFWENLYQLTLRAAGKTYMIFFVLVIFLGSFYLINLILA
VVAMAYEEQNQATLEEAEQKEAEFQQMIEQLKKQQEAAQQAATATASEHSREPSAAGRLS
DSSSEASKLSSKSAKERRNRRKKRKQKEQSGGEEKDEDEFQKSESEDSIRRKGFRFSIEG
NRLTYEKRYSSPHQSLLSIRGSLFSPRRNSRTSLFSFRGRAKDVGSENDFADDEHSTFED
NESRRDSLFVPRRHGERRNSNLSQTSRSSRMLAVFPANGKMHSTVDCNGVVSLVGGPSVP
TSPVGQLLPEVIIDKPATDDNGTTTETEMRKRRSSSFHVSMDFLEDPSQRQRAMSIASIL
TNTVEELEESRQKCPPCWYKFSNIFLIWDCSPYWLKVKHVVNLVVMDPFVDLAITICIVL
NTLFMAMEHYPMTDHFNNVLTVGNLVFTGIFTAEMFLKIIAMDPYYYFQEGWNIFDGFIV
TLSLVELGLANVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAII
VFIFAVVGMQLFGKSYKDCVCKIASDCQLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCM
EVAGQAMCLTVFMMVMVIGNLVVLNLFLALLLSSFSADNLAATDDDNEMNNLQIAVDRMH
KGVAYVKRKIYEFIQQSFIRKQKILDEIKPLDDLNNKKDSCMSNHTAEIGKDLDYLKDVN
GTTSGIGTGSSVEKYIIDESDYMSFINNPSLTVTVPIAVGESDFENLNTEDFSSESDLEE
SKEKLNESSSSSEGSTVDIGAPVEEQPVVEPEETLEPEACFTEGCVQRFKCCQINVEEGR
GKQWWNLRRTCFRIVEHNWFETFIVFMILLSSGALAFEDIYIDQRKTIKTMLEYADKVFT
YIFILEMLLKWVAYGYQTYFTNAWCWLDFLIVDVSLVSLTANALGYSELGAIKSLRTLRA
LRPLRALSRFEGMRVVVNALLGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYHCINTT
TGDRFDIEDVNNHTDCLKLIERNETARWKNVKVNFDNVGFGYLSLLQVATFKGWMDIMYA
AVDSRNVELQPKYEESLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFM
TEEQKKYYNAMKKLGSKKPQKPIPRPGNKFQGMVFDFVTRQVFDISIMILICLNMVTMMV
ETDDQSEYVTTILSRINLVFIVLFTGECVLKLISLRHYYFTIGWNIFDFVVVILSIVGMF
LAELIEKYFVSPTLFRVIRLARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLV
MFIYAIFGMSNFAYVKREVGIDDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSKPPD
CDPNKVNPGSSVKGDCGNPSVGIFFFVSYIIISFLVVVNMYIAVILENFSVATEESAEPL
SEDDFEMFYEVWEKFDPDATQFMEFEKLSQFAAALEPPLNLPQPNKLQLIAMDLPMVSGD
RIHCLDILFAFTKRVLGESGEMDALRIQMEERFMASNPSKVSYQPITTTLKRKQEEVSAV
IIQRAYRRHLLKRTVKQASFTYNKNKIKGGANLLIKEDMIIDRINENSITEKTDLTMSTA
ACPPSYDRVTKPIVEKHEQEGKDEKAKGK
Drugs and Mode of Action
Drug(s) Benzocaine Drug Info Approved Anesthesia [1]
Butacaine Drug Info Approved Pain [2]
Carbamazepine Drug Info Approved Epilepsy [3], [4]
Eslicarbazepine Drug Info Approved Seizures [5], [6]
Levobupivacaine Drug Info Approved Anesthesia [7], [8]
LIDOFLAZINE Drug Info Approved Angina pectoris [2]
LOMERIZINE Drug Info Approved Migraine [9], [2]
Mepivacaine Drug Info Approved Local or regional analgesia and anesthesia [2]
Oxybuprocaine Drug Info Approved Anesthesia [10], [11]
Pachycarpine Drug Info Approved Oxytocic [2]
Permethrin Drug Info Approved Infections with sarcoptes scabiei [12], [2]
Phenacemide Drug Info Approved Epilepsy [13], [14]
Phenytoin Drug Info Approved Seizures occurring during or following neurosurgery [2]
Pilsicainide Drug Info Approved Heart arrhythmia [2]
Pirmenol Drug Info Approved Heart arrhythmia [2]
Rufinamide Drug Info Approved Seizures associated with lennox-Gastaut syndrome [15], [16], [2]
Zonisamide Drug Info Approved Epilepsy [17], [18]
Rufinamide Drug Info Approved (orphan drug) Epilepsy [19], [16]
I.V. carbamazepine Drug Info NDA filed Type 1 diabetes [20]
Carisbamate Drug Info Phase 3 Epilepsy; Focal; Seizure disorder [21]
Intravenous carbamazepine Drug Info Phase 3 Gastric cancer [22]
Ralfinamide Drug Info Phase 3 Neuropathic pain [23]
BN82451 Drug Info Phase 2 Parkinson's disease [24]
COL-1077 Drug Info Phase 2 Pain [25]
CROBENETINE HYDROCHLORIDE Drug Info Phase 2 Pain [26]
GSK1014802 Drug Info Phase 2 Bipolar disorder [27]
GSK2339345 Drug Info Phase 2 Cough [28]
NS-7 Drug Info Phase 2 Nerve injury [29]
Phenylbutyrate Drug Info Phase 2 Urea cycle disorders [30], [31]
SMP-986 Drug Info Phase 2 Overactive bladder disorder [32]
TV-45070 Drug Info Phase 2 Osteoarthritis [33]
P-552-02 Drug Info Phase 1/2 Cystic fibrosis [34], [35]
ADCI Drug Info Phase 1 Epileptic seizures [36]
AZD-3161 Drug Info Phase 1 Peripheral neuropathy [37]
BDD-10103 Drug Info Phase 1 Pain [38]
NW-3509 Drug Info Phase 1 Schizophrenia [39]
LUBELUZOLE Drug Info Discontinued in Preregistration Neurological disease [40]
Bidisomide Drug Info Discontinued in Phase 3 Heart arrhythmia [41]
Licarbazepine Drug Info Discontinued in Phase 3 Bipolar disorder [42]
4030W92 Drug Info Discontinued in Phase 2 Pain [43]
4991W93 Drug Info Discontinued in Phase 2 Migraine [44]
534U87 Drug Info Discontinued in Phase 2 Epileptic seizures [45]
Levosemotiadil Drug Info Discontinued in Phase 2 Cardiac arrhythmias [46]
Org-7797 Drug Info Discontinued in Phase 2 Cardiac arrhythmias [47]
Pentisomide Drug Info Discontinued in Phase 2 Heart arrhythmia [48]
Pyrazinoylguanidine Drug Info Discontinued in Phase 2 Diabetes [49]
RSD-921 Drug Info Discontinued in Phase 2 Anesthesia [50]
SILPERISONE HYDROCHLORIDE Drug Info Discontinued in Phase 2 Spasm [51]
SIPATRIGINE Drug Info Discontinued in Phase 2 Neurological disease [52]
SOLPECAINOL HYDROCHLORIDE Drug Info Discontinued in Phase 2 Cardiac arrhythmias [53]
AMELTOLIDE Drug Info Discontinued in Phase 1 Epileptic seizures [54]
Artilide Drug Info Discontinued in Phase 1 Cardiac arrhythmias [55]
AWD-140-190 Drug Info Discontinued in Phase 1 Epileptic seizures [56]
SL-90.0571 Drug Info Discontinued in Phase 1 Epilepsy [57]
A-76895 Drug Info Terminated Epilepsy [58]
AM-66 Drug Info Terminated Pain [59]
BDF-9148 Drug Info Terminated Cardiac failure [60]
Berlafenone Drug Info Terminated Heart arrhythmia [61]
BW-1003C87 Drug Info Terminated Cerebrovascular ischaemia [62]
DPI-201-106 Drug Info Terminated Cardiovascular disorder [63]
E-2070 Drug Info Terminated Neuropathic pain [64]
GE-68 Drug Info Terminated Heart arrhythmia [65]
PD-85639 Drug Info Terminated Discovery agent [66]
R-59494 Drug Info Terminated Ischemia [67]
Ralitoline Drug Info Terminated Epilepsy [68]
Recainam Drug Info Terminated Heart arrhythmia [69]
RP-66055 Drug Info Terminated Cerebral infarction [70]
RS-2135 Drug Info Terminated Heart arrhythmia [71]
SRSC-355 Drug Info Terminated Neuropathic pain [72]
U-54494A Drug Info Terminated Epilepsy [73]
U-92032 Drug Info Terminated Discovery agent [74]
Inhibitor 2-(1-Pentyl-hexyl)-4-phenyl-1H-imidazole Drug Info [75]
2-Hexyl-4-(4-isobutyl-phenyl)-1H-imidazole Drug Info [75]
2-Hydroxy-2-phenyl-nonanoic acid amide Drug Info [76]
4-Biphenyl-4-yl-2-(1-pentyl-hexyl)-1H-imidazole Drug Info [75]
4-Biphenyl-4-yl-2-(1-propyl-butyl)-1H-imidazole Drug Info [75]
4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazole Drug Info [75]
4-Biphenyl-4-yl-2-hexyl-1H-imidazole Drug Info [75]
4-Biphenyl-4-yl-2-methyl-1H-imidazole Drug Info [75]
5-Ethyl-3-methyl-5-phenyl-oxazolidine-2,4-dione Drug Info [77]
5-Heptyl-5-phenyl-imidazolidine-2,4-dione Drug Info [76]
5-Hexyl-5-phenyl-imidazolidine-2,4-dione Drug Info [76]
5-Nonyl-5-phenyl-imidazolidine-2,4-dione Drug Info [76]
BW-202W92 Drug Info [78]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info [79]
L-741742 Drug Info [80]
LIDOFLAZINE Drug Info [81]
LOMERIZINE Drug Info [79]
LUBELUZOLE Drug Info [79]
PD-85639 Drug Info [79]
SIPATRIGINE Drug Info [79]
TV-45070 Drug Info [82]
U-92032 Drug Info [83]
Modulator 4030W92 Drug Info [84], [2]
4991W93 Drug Info [85]
534U87 Drug Info [86]
A-76895 Drug Info [87]
ADCI Drug Info [36]
AMELTOLIDE Drug Info [88], [2]
Artilide Drug Info [89], [2]
AWD-140-190 Drug Info [90]
AZD-3161 Drug Info [91]
BDD-10103 Drug Info [92]
BDF-9148 Drug Info [93]
Berlafenone Drug Info [94]
Bidisomide Drug Info [95]
Butacaine Drug Info [96], [2]
BW-1003C87 Drug Info [97]
Carbamazepine Drug Info [98]
DPI-201-106 Drug Info [99]
GE-68 Drug Info [100]
GSK2339345 Drug Info [101]
I.V. carbamazepine Drug Info [98]
Intravenous carbamazepine Drug Info [98]
Levosemotiadil Drug Info [102]
NS-7 Drug Info [29]
Org-7797 Drug Info [103]
Pachycarpine Drug Info [104], [105]
Pentisomide Drug Info [106]
Pilsicainide Drug Info [107], [2]
Pirmenol Drug Info [108], [2]
Pyrazinoylguanidine Drug Info [109]
R-59494 Drug Info [110]
Ralitoline Drug Info [111]
Recainam Drug Info [112]
RP-66055 Drug Info [113]
RS-2135 Drug Info [114]
RSD-921 Drug Info [115]
SILPERISONE HYDROCHLORIDE Drug Info [116], [2]
SL-90.0571 Drug Info [94]
SOLPECAINOL HYDROCHLORIDE Drug Info [117], [2]
SRSC-355 Drug Info [118]
U-54494A Drug Info [119]
Blocker AM-66 Drug Info [87]
Benzocaine Drug Info [120]
BN82451 Drug Info [121]
Carisbamate Drug Info [122], [19], [21]
E-2070 Drug Info [123]
Eslicarbazepine Drug Info [21]
GSK1014802 Drug Info [124]
Levobupivacaine Drug Info [125]
Licarbazepine Drug Info [42]
Mepivacaine Drug Info [125]
NW-3509 Drug Info [126]
Oxybuprocaine Drug Info [127]
P-552-02 Drug Info [128]
Permethrin Drug Info [129]
Phenacemide Drug Info [130]
Phenylbutyrate Drug Info [30]
Phenytoin Drug Info [131]
Ralfinamide Drug Info [23]
Rufinamide Drug Info [122]
Saxitoxin Drug Info [132]
Zonisamide Drug Info [133]
Antagonist COL-1077 Drug Info [134]
CROBENETINE HYDROCHLORIDE Drug Info [135], [2]
SMP-986 Drug Info [136]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Dopaminergic synapse
Reactome Interaction between L1 and Ankyrins
References
REF 1Double-blind, randomized, placebo-controlled clinical trials with non-prescription medications for the treatment of obesity. Obes Res. 1999 Jul;7(4):370-8.
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3Thirty years of clinical experience with carbamazepine in the treatment of bipolar illness: principles and practice. CNS Drugs. 2007;21(1):47-71.
REF 4(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: 5339).
REF 52013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
REF 6(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: 7350).
REF 7FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020997.
REF 8(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: 7211).
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002033)
REF 10(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: 7123).
REF 11Drug information of Oxybuprocaine, 2008. eduDrugs.
REF 12FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074806.
REF 13FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 007707.
REF 14(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: 7265).
REF 152008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
REF 16(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: 7470).
REF 17Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54.
REF 18(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: 7047).
REF 19Pharmacological management of epilepsy: recent advances and future prospects. Drugs. 2008;68(14):1925-39.
REF 20Clinical pipeline report, company report or official report of Lundbeck.
REF 21Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43. Epub 2008 Nov 12.
REF 22ClinicalTrials.gov (NCT01128959) Study to Assess the Safety and Tolerability of Intravenous Carbamazepine in Adults With Epilepsy. U.S. National Institutes of Health.
REF 23Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
REF 24ClinicalTrials.gov (NCT02231580) Study Exploring Safety, Pharmacokinetic and Pharmacodynamic of BN82451 in Male Huntington's Disease Patients. U.S. National Institutes of Health.
REF 25ClinicalTrials.gov (NCT02465320) COL-1077 (Lidocaine Bioadhesive Gel, 10%) in Women Undergoing Transvaginal Pipelle-Directed Endometrial Biopsy.
REF 26ClinicalTrials.gov (NCT02251197) Safety and Tolerability of BIII 890 in Patients With Acute Ischemic Stroke. U.S. National Institutes of Health.
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027679)
REF 28ClinicalTrials.gov (NCT01899768) GSK2339345 Hypertussive Challenge Study. U.S. National Institutes of Health.
REF 29Preferential inhibition by a novel Na(+)/Ca(2+) channel blocker NS-7 of severe to mild hypoxic injury in rat cerebrocortical slices: A possible involvement of a highly voltage-dependent blockade of Ca(2+) channel. J Pharmacol Exp Ther. 2000 May;293(2):522-9.
REF 30Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
REF 31(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: 8480).
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022820)
REF 33ClinicalTrials.gov (NCT02068599) A Study to Evaluate the Safety and Efficacy of Topically Applied TV-45070 Ointment) in Participants With Primary Osteoarthritis (OA) Affecting a Single Knee. U.S. National Institutes of Health.
REF 34(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: 4280).
REF 35ClinicalTrials.gov (NCT01369589) An Evaluation of the Impact of a Single Dose of P-552 on Oral Mucosal Wetness. U.S. National Institutes of Health.
REF 36The anticonvulsant SGB-017 (ADCI) blocks voltage-gated sodium channels in rat and human neurons: comparison with carbamazepine. Epilepsia. 2000 Mar;41(3):263-70.
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033244)
REF 38Clinical pipeline report, company report or official report of Birds Pharma AG.
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026870)
REF 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005388)
REF 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000174)
REF 42Emerging drugs for bipolar disorder. Expert Opin Emerg Drugs. 2006 Nov;11(4):621-34.
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006453)
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009029)
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006296)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005516)
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000279)
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000271)
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002279)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006443)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002660)
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003158)
REF 54Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008003)
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002256)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005495)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002249)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002237)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019471)
REF 60Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008457)
REF 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000213)
REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002740)
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000134)
REF 64Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019940)
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001596)
REF 66Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002730)
REF 67Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002300)
REF 68Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003367)
REF 69Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000248)
REF 70Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003439)
REF 71Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001212)
REF 72Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018179)
REF 73Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002236)
REF 74Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004258)
REF 75Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
REF 76J Med Chem. 1999 May 6;42(9):1537-45.Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.
REF 77J Med Chem. 1989 Jul;32(7):1577-80.Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models.
REF 78J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones.
REF 79J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
REF 80J Med Chem. 1999 Jul 15;42(14):2706-15.1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
REF 81J Med Chem. 1994 Jan 21;37(2):268-74.Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.
REF 82Clinical pipeline report, company report or official report of Xenon Pharma.
REF 83J Med Chem. 2000 Sep 7;43(18):3372-6.Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.
REF 84Lack of effect of two oral sodium channel antagonists, lamotrigine and 4030W92, on intradermal capsaicin-induced hyperalgesia model. Pharmacol Biochem Behav. 2004 Jun;78(2):349-55.
REF 85CGRP and its receptors provide new insights into migraine pathophysiology. Nat Rev Neurol. 2010 Oct;6(10):573-82.
REF 86The anticonvulsant BW534U87 depresses epileptiform activity in rat hippocampal slices by an adenosine-dependent mechanism and through inhibition of voltage-gated Na+ channels. Br J Pharmacol. 1999 Nov;128(5):1011-20.
REF 87CA patent application no. 849505, Sodium channel blockers reduce glucagon secretion.
REF 88Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant. J Med Chem. 1991 Apr;34(4):1253-7.
REF 89Potassium channel blockers as antiarrhythmic drugs. Drug Development Research Volume 33, Issue 3, pages 235-249, November 1994.
REF 90Effects of AWD 140-190 on stimulus-induced field potentials and on different patterns of epileptiform activity induced by low calcium or low magnesium in rat entorhinal cortex hippocampal slices. Epilepsy Res. 1997 Dec;29(1):59-69.
REF 91Recent progress in sodium channel modulators for pain.Bioorganic & Medicinal Chemistry Letters Volume 24, Issue 16, 15 August 2014, Pages 3690-3699.
REF 92Clinical pipeline report, company report or official report of Birds Pharma AG.
REF 93The relaxing effect of BDF 9148 on the KCl-contracted aorta isolated from normo- and hyper-tensive rats. Naunyn Schmiedebergs Arch Pharmacol. 1998 Feb;357(2):126-32.
REF 94WO patent application no. 19990639849, Novel sodium channel drugs and uses.
REF 95Bidisomide (SC-40230), a new antiarrhythmic agent: initial study of tolerability and pharmacokinetics. Clin Pharmacol Ther. 1992 Apr;51(4):371-8.
REF 96WO patent application no. 2008,0857,11, Synergy of sodium channel blockers and calcium channel blockers.
REF 97The pyrimidine-derivative, BW1003C87, protects CA1 and striatal neurons following transient severe forebrain ischaemia in rats. A microdialysis and histological study. Neuroscience. 1993 Sep;56(1):93-9.
REF 98Sidedness of carbamazepine accessibility to voltage-gated sodium channels. Mol Pharmacol. 2014 Feb;85(2):381-7.
REF 99Interaction between DPI 201-106 enantiomers at the cardiac sodium channel. Mol Pharmacol. 1990 Jan;37(1):17-24.
REF 100Electrophysiological properties of the propafenone-analogue GE 68 (1-[3-(phenylethyl)-2-benzofuryl]-2-(propylamino)-ethanol) in isolated preparations and ventricular myocytes of guinea-pig hearts. Naunyn Schmiedebergs Arch Pharmacol. 1997 Feb;355(2):230-8.
REF 101ClinicalTrials.gov (NCT01494636) The Safety, Tolerability, PK and PD of GSK2339345 in Healthy Subjects. U.S. National Institutes of Health.
REF 102Binding study of semotiadil and levosemotiadil with alpha(1)-acid glycoprotein using high-performance frontal analysis. Anal Biochem. 1999 Oct 1;274(1):27-33.
REF 103Electrophysiologic effects of Org 7797, a new steroidal antiarrhythmic agent: comparison with class 1a, 1b, and 1c drugs. J Cardiovasc Pharmacol. 1989 Aug;14(2):205-12.
REF 104The role of weeds as sources of pharmaceuticals. J Ethnopharmacol. 2004 Jun;92(2-3):163-6.
REF 105Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
REF 106Antiarrhythmic effect related to the plasma concentration of pentisomide in vivo and the antiarrhythmic-concentration relationship in vitro. Drugs Exp Clin Res. 1995;21(4):145-51.
REF 107A sodium channel blocker, pilsicainide, produces atrial post-repolarization refractoriness through the reduction of sodium channel availability. Tohoku J Exp Med. 2011;225(1):35-42.
REF 108Pirmenol, a new antiarrhythmic drug with potassium- and sodium-channel blocking activity; a voltage-clamp study in rabbit Purkinje fibres. Naunyn Schmiedebergs Arch Pharmacol. 1990 May;341(5):462-71.
REF 109Design, synthesis, and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis. J Med Chem. 2006 Jul 13;49(14):4098-115.
REF 110Veratridine activates a silent sodium channel in rat isolated aorta. Eur J Pharmacol. 1992 Aug 25;219(2):253-9.
REF 111Anticonvulsant and sodium channel blocking effects of ralitoline in different screening models. Naunyn Schmiedebergs Arch Pharmacol. 1992 Oct;346(4):442-52.
REF 112Effects of renal function on recainam pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther. 1995 May;57(5):492-8.
REF 113Synthesis, anticonvulsant and neuroprotective activities of RP 66055, a riluzole derivative. Bioorg Med Chem. 1994 Aug;2(8):793-8.
REF 114Electrophysiologic effects of RS-2135, a new antiarrhythmic compound, on canine Purkinje fibers. J Cardiovasc Pharmacol. 1992 Dec;20(6):955-60.
REF 115Molecular analysis of the Na+ channel blocking actions of the novel class I anti-arrhythmic agent RSD 921. Br J Pharmacol. 1999 May;127(1):9-18.
REF 116Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J Pharmacol Exp Ther. 2005 Dec;315(3):1237-46. Epub 2005 Aug 26.
REF 117US patent application no. 2002,0102,217, Diagnostic,therapeutic agents.
REF 118WO patent application no. 2013,0439,25, Sodium channel blockers reduce glucagon secretion.
REF 119U-54494A: a unique anticonvulsant related to kappa opioid agonists. J Pharmacol Exp Ther. 1987 Nov;243(2):542-7.
REF 120Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels. Circ Res. 2008 Jan 4;102(1):86-94. Epub 2007 Oct 25.
REF 121Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97.
REF 122Emerging drugs for epilepsy. Expert Opin Emerg Drugs. 2007 Sep;12(3):407-22.
REF 123Emerging therapies for neuropathic pain. Expert Opin Emerg Drugs. 2005 Feb;10(1):95-108.
REF 124Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 125Block of neuronal tetrodotoxin-resistant Na+ currents by stereoisomers of piperidine local anesthetics. Anesth Analg. 2000 Dec;91(6):1499-505.
REF 126Clinical pipeline report, company report or official report of Newron.
REF 127Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats. Neurosci Lett. 2009 May 1;454(3):249-53. Epub 2009 Mar 11.
REF 128US patent application no. 2014,0221,286, Sodium channel blockers reduce glucagon secretion.
REF 129In vitro assays for repellents and deterrents for ticks: differing effects of products when tested with attractant or arrestment stimuli. Med Vet Entomol. 2003 Dec;17(4):370-8.
REF 130How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 131Lacosamide: 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 132Effect of neurotoxins on the electrical activity and contraction of the heart muscle. C R Seances Soc Biol Fil. 1997;191(3):451-71.
REF 133Antiepileptic drugs and relapse after epilepsy surgery. Epileptic Disord. 2008 Sep;10(3):193-8.
REF 134Clinical pipeline report, company report or official report of Columbia Laboratories.
REF 135Analgesic activity of a novel use-dependent sodium channel blocker, crobenetine, in mono-arthritic rats. Br J Pharmacol. 2001 Dec;134(8):1742-8.
REF 136DUAL INHIBITION OF Na+-CHANNEL AND MUSCARINIC RECEPTORS BY SMP-986 EFFICIENTLY IMPROVED VOIDING FUNCTION COMPARED TO ANTI-MUSCARINIC AGENTS IN TWO CONSCIOUS RAT MODELS OF DETRUSOR OVERACTIVITY. The Journal of Urology Volume 179, Issue 4, Supplement, April 2008, Pages 129.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.