Target Information
Target General Infomation | |||||
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Target ID |
T43739
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Former ID |
TTDS00514
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Target Name |
Voltage-gated sodium channel subunit alpha Nav1.8
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Gene Name |
SCN10A
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Synonyms |
PN3; SNS; TTX-R sodium channel; TTX-R/NaV1.8; Transient tetrodotoxin-resistant Na+ current; Voltage-gated sodium channel NaV1.8; SCN10A
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Target Type |
Successful
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Disease | Asthma [ICD10: J45] | ||||
Anesthesia [ICD9: 338; ICD10: R20.0] | |||||
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0] | |||||
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] | |||||
Spinal anesthesia [ICD9: 338; ICD10: R20.0] | |||||
Function |
Tetrodotoxin-resistant channel that 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 sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
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BioChemical Class |
Sodium channel
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Target Validation |
T43739
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UniProt ID | |||||
Sequence |
MEFPIGSLETNNFRRFTPESLVEIEKQIAAKQGTKKAREKHREQKDQEEKPRPQLDLKAC
NQLPKFYGELPAELIGEPLEDLDPFYSTHRTFMVLNKGRTISRFSATRALWLFSPFNLIR RTAIKVSVHSWFSLFITVTILVNCVCMTRTDLPEKIEYVFTVIYTFEALIKILARGFCLN EFTYLRDPWNWLDFSVITLAYVGTAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALI HSVKKLADVTILTIFCLSVFALVGLQLFKGNLKNKCVKNDMAVNETTNYSSHRKPDIYIN KRGTSDPLLCGNGSDSGHCPDGYICLKTSDNPDFNYTSFDSFAWAFLSLFRLMTQDSWER LYQQTLRTSGKIYMIFFVLVIFLGSFYLVNLILAVVTMAYEEQNQATTDEIEAKEKKFQE ALEMLRKEQEVLAALGIDTTSLHSHNGSPLTSKNASERRHRIKPRVSEGSTEDNKSPRSD PYNQRRMSFLGLASGKRRASHGSVFHFRSPGRDISLPEGVTDDGVFPGDHESHRGSLLLG GGAGQQGPLPRSPLPQPSNPDSRHGEDEHQPPPTSELAPGAVDVSAFDAGQKKTFLSAEY LDEPFRAQRAMSVVSIITSVLEELEESEQKCPPCLTSLSQKYLIWDCCPMWVKLKTILFG LVTDPFAELTITLCIVVNTIFMAMEHHGMSPTFEAMLQIGNIVFTIFFTAEMVFKIIAFD PYYYFQKKWNIFDCIIVTVSLLELGVAKKGSLSVLRSFRLLRVFKLAKSWPTLNTLIKII GNSVGALGNLTIILAIIVFVFALVGKQLLGENYRNNRKNISAPHEDWPRWHMHDFFHSFL IVFRILCGEWIENMWACMEVGQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTA PEDDGEVNNLQVALARIQVFGHRTKQALCSFFSRSCPFPQPKAEPELVVKLPLSSSKAEN HIAANTARGSSGGLQAPRGPRDEHSDFIANPTVWVSVPIAEGESDLDDLEDDGGEDAQSF QQEVIPKGQQEQLQQVERCGDHLTPRSPGTGTSSEDLAPSLGETWKDESVPQVPAEGVDD TSSSEGSTVDCLDPEEILRKIPELADDLEEPDDCFTEGCIRHCPCCKLDTTKSPWDVGWQ VRKTCYRIVEHSWFESFIIFMILLSSGSLAFEDYYLDQKPTVKALLEYTDRVFTFIFVFE MLLKWVAYGFKKYFTNAWCWLDFLIVNISLISLTAKILEYSEVAPIKALRTLRALRPLRA LSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFWRCINYTDGEFSL VPLSIVNNKSDCKIQNSTGSFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDSR EVNMQPKWEDNVYMYLYFVIFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQK KYYNAMKKLGSKKPQKPIPRPLNKFQGFVFDIVTRQAFDITIMVLICLNMITMMVETDDQ SEEKTKILGKINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVVLSIASLIFSAIL KSLQSYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMFI YSIFGMSSFPHVRWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDP NLPNSNGTRGDCGSPAVGIIFFTTYIIISFLIMVNMYIAVILENFNVATEESTEPLSEDD FDMFYETWEKFDPEATQFITFSALSDFADTLSGPLRIPKPNRNILIQMDLPLVPGDKIHC LDILFAFTKNVLGESGELDSLKANMEEKFMATNLSKSSYEPIATTLRWKQEDISATVIQK AYRSYVLHRSMALSNTPCVPRAEEEAASLPDEGFVAFTANENCVLPDKSETASATSFPPS YESVTRGLSDRVNMRTSSSIQNEDEATSMELIAPGP |
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Structure |
1BYY
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Drugs and Mode of Action | |||||
Drug(s) | Bupivacaine | Drug Info | Approved | Anesthesia | [538239], [539524] |
Proparacaine | Drug Info | Approved | Anesthesia | [538162], [542303] | |
Ropivacaine | Drug Info | Approved | Anesthesia | [538331], [542591] | |
Tetracaine | Drug Info | Approved | Spinal anesthesia | [535622] | |
Tetracaine | Drug Info | Phase 2 | Pain | [551871] | |
PF-01247324 | Drug Info | Phase 1 | Pain | [543182] | |
SPI-860 | Drug Info | Phase 1 | Neuropathic pain | [536374] | |
Corus 1030 | Drug Info | Discontinued in Phase 2 | Asthma | [547604] | |
SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disease | [545614] | |
Inhibitor | 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | [529491] | ||
5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide | Drug Info | [531169] | |||
A-803467 | Drug Info | [536866] | |||
BW-202W92 | Drug Info | [530055] | |||
Mu O-conotoxin | Drug Info | [535930] | |||
N-(2-chlorobenzyl)-5-(4-chlorophenyl)nicotinamide | Drug Info | [531169] | |||
N-benzyl-5-(4-chlorophenyl)nicotinamide | Drug Info | [531169] | |||
SCH-725737 | Drug Info | [529019] | |||
SCH-725739 | Drug Info | [529019] | |||
SIPATRIGINE | Drug Info | [530055] | |||
SPI-860 | Drug Info | [536374] | |||
Tetracaine | Drug Info | [535913] | |||
Activator | batrachotoxin | Drug Info | [527277] | ||
veratridine | Drug Info | [529119] | |||
Modulator | Bupivacaine | Drug Info | [556264] | ||
Corus 1030 | Drug Info | [527078] | |||
Proparacaine | Drug Info | [556264] | |||
Ropivacaine | Drug Info | [556264] | |||
Blocker | CR-4892 | Drug Info | [543885] | ||
PF-01247324 | Drug Info | [544467] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
Reactome | Interaction between L1 and Ankyrins | ||||
References | |||||
Ref 535622 | Evaluation of a novel topical anesthetic agent for cutaneous laser resurfacing: a randomized comparison study. Dermatol Surg. 2002 Nov;28(11):1004-6; discussion 1006. | ||||
Ref 538162 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040074. | ||||
Ref 538239 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071810. | ||||
Ref 538331 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 078601. | ||||
Ref 539524 | (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: 2397). | ||||
Ref 542303 | (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: 7283). | ||||
Ref 542591 | (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: 7602). | ||||
Ref 543182 | (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: 8521). | ||||
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 527078 | Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine. Br J Pharmacol. 2004 Jun;142(3):576-84. Epub 2004 May 17. | ||||
Ref 527277 | The poison Dart frog's batrachotoxin modulates Nav1.8. FEBS Lett. 2004 Nov 5;577(1-2):245-8. | ||||
Ref 529019 | Bioorg Med Chem Lett. 2007 Oct 15;17(20):5543-7. Epub 2007 Aug 16.Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis. | ||||
Ref 529119 | A comparison of the effects of veratridine on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels in isolated rat dorsal root ganglion neurons. Pflugers Arch. 2008 Feb;455(5):929-38. Epub 2007 Oct 26. | ||||
Ref 529491 | Bioorg 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 530055 | J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. | ||||
Ref 531169 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. Epub 2010 Sep 18.Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. | ||||
Ref 535913 | Heterologous expression and functional analysis of rat Nav1.8 (SNS) voltage-gated sodium channels in the dorsal root ganglion neuroblastoma cell line ND7-23. Neuropharmacology. 2004 Mar;46(3):425-38. | ||||
Ref 535930 | Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian sensory neurons. J Biol Chem. 2004 Jun 11;279(24):25774-82. Epub 2004 Mar 24. | ||||
Ref 536866 | Sensory neuron voltage-gated sodium channels as analgesic drug targets. Curr Opin Neurobiol. 2008 Aug;18(4):383-8. | ||||
Ref 543885 | (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. (Target id: 585). |
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