Target Information
Target General Infomation | |||||
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Target ID |
T29303
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Former ID |
TTDS00155
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Target Name |
Sodium channel
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Gene Name |
SCN1A
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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
|
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Target Type |
Successful
|
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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] | |||||
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47] | |||||
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81] | |||||
Oxytocic [ICD10: O00-O99] | |||||
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 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] | |||||
Seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56] | |||||
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.
|
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BioChemical Class |
Sodium channel
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Target Validation |
T29303
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UniProt ID | |||||
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 |
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Drugs and Mode of Action | |||||
Drug(s) | Benzocaine | Drug Info | Approved | Anesthesia | [534892] |
Butacaine | Drug Info | Approved | Pain | [551871] | |
Carbamazepine | Drug Info | Approved | Epilepsy | [528598], [540778] | |
Eslicarbazepine | Drug Info | Approved | Seizures | [532651], [542371] | |
Levobupivacaine | Drug Info | Approved | Anesthesia | [538559], [542226] | |
LIDOFLAZINE | Drug Info | Approved | Angina pectoris | [551871] | |
LOMERIZINE | Drug Info | Approved | Migraine | [545070], [551871] | |
Mepivacaine | Drug Info | Approved | Local or regional analgesia and anesthesia | [551871] | |
Oxybuprocaine | Drug Info | Approved | Anesthesia | [542131], [550739] | |
Pachycarpine | Drug Info | Approved | Oxytocic | [551871] | |
Permethrin | Drug Info | Approved | Infections with sarcoptes scabiei | [538286], [551871] | |
Phenacemide | Drug Info | Approved | Epilepsy | [538401], [542284] | |
Phenytoin | Drug Info | Approved | Seizures occurring during or following neurosurgery | [551871] | |
Pilsicainide | Drug Info | Approved | Heart arrhythmia | [551871] | |
Pirmenol | Drug Info | Approved | Heart arrhythmia | [551871] | |
Rufinamide | Drug Info | Approved | Seizures associated with lennox-Gastaut syndrome | [529941], [542495], [551871] | |
Zonisamide | Drug Info | Approved | Epilepsy | [536756], [542058] | |
Rufinamide | Drug Info | Approved (orphan drug) | Epilepsy | [536845], [542495] | |
I.V. carbamazepine | Drug Info | NDA filed | Type 1 diabetes | [551104] | |
Carisbamate | Drug Info | Phase 3 | Epilepsy; Focal; Seizure disorder | [536934] | |
Intravenous carbamazepine | Drug Info | Phase 3 | Gastric cancer | [523052] | |
Ralfinamide | Drug Info | Phase 3 | Neuropathic pain | [536374] | |
BN82451 | Drug Info | Phase 2 | Parkinson's disease | [524900] | |
COL-1077 | Drug Info | Phase 2 | Pain | [525222] | |
CROBENETINE HYDROCHLORIDE | Drug Info | Phase 2 | Pain | [524933] | |
GSK1014802 | Drug Info | Phase 2 | Bipolar disorder | [548689] | |
GSK2339345 | Drug Info | Phase 2 | Cough | [524368] | |
NS-7 | Drug Info | Phase 2 | Nerve injury | [525754] | |
Phenylbutyrate | Drug Info | Phase 2 | Urea cycle disorders | [536447], [543164] | |
SMP-986 | Drug Info | Phase 2 | Overactive bladder disorder | [548182] | |
TV-45070 | Drug Info | Phase 2 | Osteoarthritis | [524653] | |
P-552-02 | Drug Info | Phase 1/2 | Cystic fibrosis | [467618], [523506] | |
ADCI | Drug Info | Phase 1 | Epileptic seizures | [525718] | |
AZD-3161 | Drug Info | Phase 1 | Peripheral neuropathy | [549173] | |
BDD-10103 | Drug Info | Phase 1 | Pain | [550380] | |
NW-3509 | Drug Info | Phase 1 | Schizophrenia | [548597] | |
LUBELUZOLE | Drug Info | Discontinued in Preregistration | Neurological disease | [545928] | |
Bidisomide | Drug Info | Discontinued in Phase 3 | Heart arrhythmia | [544572] | |
Licarbazepine | Drug Info | Discontinued in Phase 3 | Bipolar disorder | [536295] | |
4030W92 | Drug Info | Discontinued in Phase 2 | Pain | [546124] | |
4991W93 | Drug Info | Discontinued in Phase 2 | Migraine | [546577] | |
534U87 | Drug Info | Discontinued in Phase 2 | Epileptic seizures | [546089] | |
Levosemotiadil | Drug Info | Discontinued in Phase 2 | Cardiac arrhythmias | [545959] | |
Org-7797 | Drug Info | Discontinued in Phase 2 | Cardiac arrhythmias | [544606] | |
Pentisomide | Drug Info | Discontinued in Phase 2 | Heart arrhythmia | [544603] | |
Pyrazinoylguanidine | Drug Info | Discontinued in Phase 2 | Diabetes | [545139] | |
RSD-921 | Drug Info | Discontinued in Phase 2 | Anesthesia | [546121] | |
SILPERISONE HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Spasm | [545273] | |
SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disease | [545614] | |
SOLPECAINOL HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Cardiac arrhythmias | [545414] | |
AMELTOLIDE | Drug Info | Discontinued in Phase 1 | Epileptic seizures | [546417] | |
Artilide | Drug Info | Discontinued in Phase 1 | Cardiac arrhythmias | [545134] | |
AWD-140-190 | Drug Info | Discontinued in Phase 1 | Epileptic seizures | [545957] | |
SL-90.0571 | Drug Info | Discontinued in Phase 1 | Epilepsy | [545133] | |
A-76895 | Drug Info | Terminated | Epilepsy | [545130] | |
AM-66 | Drug Info | Terminated | Pain | [547806] | |
BDF-9148 | Drug Info | Terminated | Cardiac failure | [546482] | |
Berlafenone | Drug Info | Terminated | Heart arrhythmia | [544579] | |
BW-1003C87 | Drug Info | Terminated | Cerebrovascular ischaemia | [545299] | |
DPI-201-106 | Drug Info | Terminated | Cardiovascular disorder | [544559] | |
E-2070 | Drug Info | Terminated | Neuropathic pain | [547856] | |
GE-68 | Drug Info | Terminated | Heart arrhythmia | [544938] | |
PD-85639 | Drug Info | Terminated | Discovery agent | [545294] | |
R-59494 | Drug Info | Terminated | Ischemia | [545149] | |
Ralitoline | Drug Info | Terminated | Epilepsy | [545466] | |
Recainam | Drug Info | Terminated | Heart arrhythmia | [544594] | |
RP-66055 | Drug Info | Terminated | Cerebral infarction | [545484] | |
RS-2135 | Drug Info | Terminated | Heart arrhythmia | [544815] | |
SRSC-355 | Drug Info | Terminated | Neuropathic pain | [547656] | |
U-54494A | Drug Info | Terminated | Epilepsy | [545129] | |
U-92032 | Drug Info | Terminated | Discovery agent | [545700] | |
Inhibitor | 2-(1-Pentyl-hexyl)-4-phenyl-1H-imidazole | Drug Info | [527102] | ||
2-Hexyl-4-(4-isobutyl-phenyl)-1H-imidazole | Drug Info | [527102] | |||
2-Hydroxy-2-phenyl-nonanoic acid amide | Drug Info | [525483] | |||
4-Biphenyl-4-yl-2-(1-pentyl-hexyl)-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-(1-propyl-butyl)-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-hexyl-1H-imidazole | Drug Info | [527102] | |||
4-Biphenyl-4-yl-2-methyl-1H-imidazole | Drug Info | [527102] | |||
5-Ethyl-3-methyl-5-phenyl-oxazolidine-2,4-dione | Drug Info | [533048] | |||
5-Heptyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
5-Hexyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
5-Nonyl-5-phenyl-imidazolidine-2,4-dione | Drug Info | [525483] | |||
BW-202W92 | Drug Info | [530055] | |||
Indol-1-yl-propyl-pyridin-4-yl-amine | Drug Info | [525961] | |||
L-741742 | Drug Info | [525540] | |||
LIDOFLAZINE | Drug Info | [533974] | |||
LOMERIZINE | Drug Info | [525961] | |||
LUBELUZOLE | Drug Info | [525961] | |||
PD-85639 | Drug Info | [525961] | |||
SIPATRIGINE | Drug Info | [525961] | |||
TV-45070 | Drug Info | [551782] | |||
U-92032 | Drug Info | [525864] | |||
Modulator | 4030W92 | Drug Info | [527123], [551871] | ||
4991W93 | Drug Info | [531151] | |||
534U87 | Drug Info | [525627] | |||
A-76895 | Drug Info | [550851] | |||
ADCI | Drug Info | [525718] | |||
AMELTOLIDE | Drug Info | [530733], [551871] | |||
Artilide | Drug Info | [550029], [551871] | |||
AWD-140-190 | Drug Info | [534534] | |||
AZD-3161 | Drug Info | [551649] | |||
BDD-10103 | Drug Info | [550379] | |||
BDF-9148 | Drug Info | [534586] | |||
Berlafenone | Drug Info | [550935] | |||
Bidisomide | Drug Info | [527361] | |||
Butacaine | Drug Info | [550133], [551871] | |||
BW-1003C87 | Drug Info | [533793] | |||
Carbamazepine | Drug Info | [532579] | |||
DPI-201-106 | Drug Info | [531461] | |||
GE-68 | Drug Info | [534330] | |||
GSK2339345 | Drug Info | [523738] | |||
I.V. carbamazepine | Drug Info | [532579] | |||
Intravenous carbamazepine | Drug Info | [532579] | |||
Levosemotiadil | Drug Info | [525617] | |||
NS-7 | Drug Info | [525754] | |||
Org-7797 | Drug Info | [532751] | |||
Pachycarpine | Drug Info | [527072], [533488] | |||
Pentisomide | Drug Info | [534070] | |||
Pilsicainide | Drug Info | [531607], [551871] | |||
Pirmenol | Drug Info | [531502], [551871] | |||
Pyrazinoylguanidine | Drug Info | [528291] | |||
R-59494 | Drug Info | [526753] | |||
Ralitoline | Drug Info | [526758] | |||
Recainam | Drug Info | [533728] | |||
RP-66055 | Drug Info | [533787] | |||
RS-2135 | Drug Info | [526657] | |||
RSD-921 | Drug Info | [525513] | |||
SILPERISONE HYDROCHLORIDE | Drug Info | [527704], [551871] | |||
SL-90.0571 | Drug Info | [550935] | |||
SOLPECAINOL HYDROCHLORIDE | Drug Info | [550841], [551871] | |||
SRSC-355 | Drug Info | [550165] | |||
U-54494A | Drug Info | [533350] | |||
Blocker | AM-66 | Drug Info | [550851] | ||
Benzocaine | Drug Info | [536525] | |||
BN82451 | Drug Info | [537349] | |||
Carisbamate | Drug Info | [536498], [536845], [536934] | |||
E-2070 | Drug Info | [536056] | |||
Eslicarbazepine | Drug Info | [536934] | |||
GSK1014802 | Drug Info | [550963] | |||
Levobupivacaine | Drug Info | [535077] | |||
Licarbazepine | Drug Info | [536295] | |||
Mepivacaine | Drug Info | [535077] | |||
NW-3509 | Drug Info | [551426] | |||
Oxybuprocaine | Drug Info | [537300] | |||
P-552-02 | Drug Info | [551923] | |||
Permethrin | Drug Info | [535876] | |||
Phenacemide | Drug Info | [536316] | |||
Phenylbutyrate | Drug Info | [536447] | |||
Phenytoin | Drug Info | [537516] | |||
Ralfinamide | Drug Info | [536374] | |||
Rufinamide | Drug Info | [536498] | |||
Saxitoxin | Drug Info | [538049] | |||
Zonisamide | Drug Info | [536848] | |||
Antagonist | COL-1077 | Drug Info | [549800] | ||
CROBENETINE HYDROCHLORIDE | Drug Info | [526220], [551871] | |||
SMP-986 | Drug Info | [551635] | |||
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 467618 | (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 523052 | ClinicalTrials.gov (NCT01128959) Study to Assess the Safety and Tolerability of Intravenous Carbamazepine in Adults With Epilepsy. U.S. National Institutes of Health. | ||||
Ref 523506 | ClinicalTrials.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 524368 | ClinicalTrials.gov (NCT01899768) GSK2339345 Hypertussive Challenge Study. U.S. National Institutes of Health. | ||||
Ref 524653 | ClinicalTrials.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 524900 | ClinicalTrials.gov (NCT02231580) Study Exploring Safety, Pharmacokinetic and Pharmacodynamic of BN82451 in Male Huntington's Disease Patients. U.S. National Institutes of Health. | ||||
Ref 524933 | ClinicalTrials.gov (NCT02251197) Safety and Tolerability of BIII 890 in Patients With Acute Ischemic Stroke. U.S. National Institutes of Health. | ||||
Ref 525222 | ClinicalTrials.gov (NCT02465320) COL-1077 (Lidocaine Bioadhesive Gel, 10%) in Women Undergoing Transvaginal Pipelle-Directed Endometrial Biopsy. | ||||
Ref 525718 | The 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 525754 | Preferential 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 528598 | Thirty years of clinical experience with carbamazepine in the treatment of bipolar illness: principles and practice. CNS Drugs. 2007;21(1):47-71. | ||||
Ref 534892 | Double-blind, randomized, placebo-controlled clinical trials with non-prescription medications for the treatment of obesity. Obes Res. 1999 Jul;7(4):370-8. | ||||
Ref 536447 | Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. | ||||
Ref 536756 | Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54. | ||||
Ref 536845 | Pharmacological management of epilepsy: recent advances and future prospects. Drugs. 2008;68(14):1925-39. | ||||
Ref 536934 | Progress 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 538286 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074806. | ||||
Ref 538401 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 007707. | ||||
Ref 538559 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020997. | ||||
Ref 540778 | (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 542058 | (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 542131 | (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 542226 | (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 542284 | (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 542371 | (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 542495 | (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 543164 | (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 544559 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000134) | ||||
Ref 544572 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000174) | ||||
Ref 544579 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000213) | ||||
Ref 544594 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000248) | ||||
Ref 544603 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000271) | ||||
Ref 544606 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000279) | ||||
Ref 544815 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001212) | ||||
Ref 544938 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001596) | ||||
Ref 545070 | 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 545129 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002236) | ||||
Ref 545130 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002237) | ||||
Ref 545133 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002249) | ||||
Ref 545134 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002256) | ||||
Ref 545139 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002279) | ||||
Ref 545149 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002300) | ||||
Ref 545273 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002660) | ||||
Ref 545294 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002730) | ||||
Ref 545299 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002740) | ||||
Ref 545414 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003158) | ||||
Ref 545466 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003367) | ||||
Ref 545484 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003439) | ||||
Ref 545614 | 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 545700 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004258) | ||||
Ref 545928 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005388) | ||||
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Ref 548689 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027679) | ||||
Ref 523738 | ClinicalTrials.gov (NCT01494636) The Safety, Tolerability, PK and PD of GSK2339345 in Healthy Subjects. U.S. National Institutes of Health. | ||||
Ref 525483 | J Med Chem. 1999 May 6;42(9):1537-45.Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. | ||||
Ref 525513 | Molecular 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 525540 | J 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 525617 | Binding 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 525627 | The 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 525718 | The 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 525754 | Preferential 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 525864 | J 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 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 526220 | Analgesic activity of a novel use-dependent sodium channel blocker, crobenetine, in mono-arthritic rats. Br J Pharmacol. 2001 Dec;134(8):1742-8. | ||||
Ref 526657 | Electrophysiologic effects of RS-2135, a new antiarrhythmic compound, on canine Purkinje fibers. J Cardiovasc Pharmacol. 1992 Dec;20(6):955-60. | ||||
Ref 526753 | Veratridine activates a silent sodium channel in rat isolated aorta. Eur J Pharmacol. 1992 Aug 25;219(2):253-9. | ||||
Ref 526758 | Anticonvulsant and sodium channel blocking effects of ralitoline in different screening models. Naunyn Schmiedebergs Arch Pharmacol. 1992 Oct;346(4):442-52. | ||||
Ref 527072 | The role of weeds as sources of pharmaceuticals. J Ethnopharmacol. 2004 Jun;92(2-3):163-6. | ||||
Ref 527102 | Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. | ||||
Ref 527123 | Lack 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 527361 | Bidisomide (SC-40230), a new antiarrhythmic agent: initial study of tolerability and pharmacokinetics. Clin Pharmacol Ther. 1992 Apr;51(4):371-8. | ||||
Ref 527704 | Tolperisone-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 528291 | Design, 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 530055 | J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. | ||||
Ref 530733 | Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant. J Med Chem. 1991 Apr;34(4):1253-7. | ||||
Ref 531151 | CGRP and its receptors provide new insights into migraine pathophysiology. Nat Rev Neurol. 2010 Oct;6(10):573-82. | ||||
Ref 531461 | Interaction between DPI 201-106 enantiomers at the cardiac sodium channel. Mol Pharmacol. 1990 Jan;37(1):17-24. | ||||
Ref 531502 | Pirmenol, 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 531607 | A 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 532579 | Sidedness of carbamazepine accessibility to voltage-gated sodium channels. Mol Pharmacol. 2014 Feb;85(2):381-7. | ||||
Ref 532751 | Electrophysiologic 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 533048 | J 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 533350 | U-54494A: a unique anticonvulsant related to kappa opioid agonists. J Pharmacol Exp Ther. 1987 Nov;243(2):542-7. | ||||
Ref 533728 | Effects of renal function on recainam pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther. 1995 May;57(5):492-8. | ||||
Ref 533787 | Synthesis, anticonvulsant and neuroprotective activities of RP 66055, a riluzole derivative. Bioorg Med Chem. 1994 Aug;2(8):793-8. | ||||
Ref 533793 | The 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 533974 | J Med Chem. 1994 Jan 21;37(2):268-74.Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. | ||||
Ref 534070 | Antiarrhythmic 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 534330 | Electrophysiological 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 534534 | Effects 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 534586 | The 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 535077 | Block of neuronal tetrodotoxin-resistant Na+ currents by stereoisomers of piperidine local anesthetics. Anesth Analg. 2000 Dec;91(6):1499-505. | ||||
Ref 535876 | In 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 536447 | Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. | ||||
Ref 536525 | Electrostatic 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 536845 | Pharmacological management of epilepsy: recent advances and future prospects. Drugs. 2008;68(14):1925-39. | ||||
Ref 536848 | Antiepileptic drugs and relapse after epilepsy surgery. Epileptic Disord. 2008 Sep;10(3):193-8. | ||||
Ref 536934 | Progress 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 537300 | Intrathecal 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 537349 | Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97. | ||||
Ref 537516 | Lacosamide: 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 538049 | Effect of neurotoxins on the electrical activity and contraction of the heart muscle. C R Seances Soc Biol Fil. 1997;191(3):451-71. | ||||
Ref 550029 | Potassium channel blockers as antiarrhythmic drugs. Drug Development Research Volume 33, Issue 3, pages 235-249, November 1994. | ||||
Ref 550133 | WO patent application no. 2008,0857,11, Synergy of sodium channel blockers and calcium channel blockers. | ||||
Ref 550165 | WO patent application no. 2013,0439,25, Sodium channel blockers reduce glucagon secretion. | ||||
Ref 551635 | DUAL 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. | ||||
Ref 551649 | Recent progress in sodium channel modulators for pain.Bioorganic & Medicinal Chemistry Letters Volume 24, Issue 16, 15 August 2014, Pages 3690-3699. |
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