Target Information
| Target General Information | Top | |||||
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| Target ID |
T43739
(Former ID: TTDS00514)
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| Target Name |
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)
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| Synonyms |
hPN3; Voltage-gated sodium channel subunit alpha Nav1.8; Sodium channel protein type X subunit alpha; Sodium channel protein type 10 subunit alpha; Peripheral nerve sodium channel 3; PN3
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| Gene Name |
SCN10A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Corneal disease [ICD-11: 9A76-9A78] | |||||
| 2 | Human immunodeficiency virus disease [ICD-11: 1C60-1C62] | |||||
| 3 | Sensation disturbance [ICD-11: MB40] | |||||
| 4 | Substance abuse [ICD-11: 6C40] | |||||
| 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 |
Voltage-gated ion channel
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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 Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Bupivacaine | Drug Info | Approved | Anaesthesia | [2], [3] | |
| 2 | Proparacaine | Drug Info | Approved | Anaesthesia | [4], [5] | |
| 3 | Rilpivirine | Drug Info | Approved | Human immunodeficiency virus infection | [6] | |
| 4 | Ropivacaine | Drug Info | Approved | Anaesthesia | [7], [8] | |
| 5 | Tetracaine | Drug Info | Approved | Spinal anesthesia | [9] | |
| 6 | Tiapride | Drug Info | Approved | Alcohol dependence | [10] | |
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | Conatumumab | Drug Info | Phase 2 | Colorectal cancer | [11] | |
| 2 | VX-150 | Drug Info | Phase 2 | Neuropathic pain | [12] | |
| 3 | DSP-2230 | Drug Info | Phase 1 | Neuropathic pain | [12], [13] | |
| 4 | PF-01247324 | Drug Info | Phase 1 | Pain | [14] | |
| 5 | VX-128 | Drug Info | Phase 1 | Pain | [12] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | Corus 1030 | Drug Info | Discontinued in Phase 2 | Asthma | [15] | |
| 2 | SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disorder | [16] | |
| Mode of Action | [+] 5 Modes of Action | + | ||||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | Bupivacaine | Drug Info | [17] | |||
| 2 | Proparacaine | Drug Info | [17] | |||
| 3 | Ropivacaine | Drug Info | [17] | |||
| 4 | Corus 1030 | Drug Info | [22], [23] | |||
| Inhibitor | [+] 16 Inhibitor drugs | + | ||||
| 1 | Rilpivirine | Drug Info | [18] | |||
| 2 | Tetracaine | Drug Info | [19] | |||
| 3 | Tiapride | Drug Info | [1] | |||
| 4 | VX-150 | Drug Info | [12] | |||
| 5 | DSP-2230 | Drug Info | [12], [13] | |||
| 6 | VX-128 | Drug Info | [12] | |||
| 7 | SIPATRIGINE | Drug Info | [24] | |||
| 8 | 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | [25] | |||
| 9 | 5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide | Drug Info | [26] | |||
| 10 | A-803467 | Drug Info | [27] | |||
| 11 | BW-202W92 | Drug Info | [24] | |||
| 12 | N-(2-chlorobenzyl)-5-(4-chlorophenyl)nicotinamide | Drug Info | [26] | |||
| 13 | N-benzyl-5-(4-chlorophenyl)nicotinamide | Drug Info | [26] | |||
| 14 | PD-32577 | Drug Info | [30] | |||
| 15 | SCH-725737 | Drug Info | [31] | |||
| 16 | SCH-725739 | Drug Info | [31] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | Conatumumab | Drug Info | [20] | |||
| Blocker | [+] 2 Blocker drugs | + | ||||
| 1 | PF-01247324 | Drug Info | [21] | |||
| 2 | CR-4892 | Drug Info | [29] | |||
| Activator | [+] 2 Activator drugs | + | ||||
| 1 | batrachotoxin | Drug Info | [28] | |||
| 2 | veratridine | Drug Info | [32] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: A-803467 | Ligand Info | |||||
| Structure Description | Human Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [33] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Human Nav1.8 with A-803467, class I | PDB:7WE4 | ||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [33] |
| PDB Sequence |
LIRRTAIKVS
127 VHSWFSLFIT137 VTILVNCVCM147 TRTDLPEKIE157 YVFTVIYTFE167 ALIKILARGF 177 CLNEFTYLRD187 PWNWLDFSVI197 TLAYVGTAID207 LRGISGLRTF217 RVLRALKTVS 227 VIPGLKVIVG237 ALIHSVKKLA247 DVTILTIFCL257 SVFALVGLQL267 FKGNLKNKCV 277 KNDMAYSSHR293 KPDIYINKRG303 TSDPLLCGNG313 SDSGHCPDGY323 ICLKTSDNPD 333 FNYTSFDSFA343 WAFLSLFRLM353 TQDSWERLYQ363 QTLRTSGKIY373 MIFFVLVIFL 383 GSFYLVNLIL393 AVVTMAYEEQ403 NQATWVKLKT656 ILFGLVTDPF666 AELTITLCIV 676 VNTIFMAMEH686 HGMSPTFEAM696 LQIGNIVFTI706 FFTAEMVFKI716 IAFDPYYYFQ 726 KKWNIFDCII736 VTVSLLELGV746 AKKGSLSVLR756 SFRLLRVFKL766 AKSWPTLNTL 776 IKIIGNSVGA786 LGNLTIILAI796 IVFVFALVGK806 QLLGENYRNN816 RKNISAPHED 826 WPRWHMHDFF836 HSFLIVFRIL846 CGEWIENMWA856 CMEVGQKSIC866 LILFLTVMVL 876 GNLVVLNLFI886 ALLLNSFFAD1136 VGWQVRKTCY1146 RIVEHSWFES1156 FIIFMILLSS 1166 GSLAFEDYYL1176 DQKPTVKALL1186 EYTDRVFTFI1196 FVFEMLLKWV1206 AYGFKKYFTN 1216 AWCWLDFLIV1226 NISLISLTAK1236 ILEYSEVAPI1246 KALRTLRALR1256 PLRALSRFEG 1266 MRVVVDALVG1276 AIPSIMNVLL1286 VCLIFWLIFS1296 IMGVNLFAGK1306 FWRCINYTDG 1316 EFSLVPLSIV1326 NNKSDCKIQN1336 STGSFFWVNV1346 KVNFDNVAMG1356 YLALLQVATF 1366 KGWMDIMYAA1376 VDSREVNMQP1386 KWEDNVYMYL1396 YFVIFIIFGG1406 FFTLNLFVGV 1416 IIDNFNQQKK1426 KLGGQDIFMT1436 EEQKKYYNAM1446 KKLGSKKPQK1456 PIPRPLNKFQ 1466 GFVFDIVTRQ1476 AFDITIMVLI1486 CLNMITMMVE1496 TDDQSEEKTK1506 ILGKINQFFV 1516 AVFTGECVMK1526 MFALRQYYFT1536 NGWNVFDFIV1546 VVLSIASLIF1556 SAILKSLQSY 1566 FSPTLFRVIR1576 LARIGRILRL1586 IRAAKGIRTL1596 LFALMMSLPA1606 LFNIGLLLFL 1616 VMFIYSIFGM1626 SSFPHVRWEA1636 GIDDMFNFQT1646 FANSMLCLFQ1656 ITTSAGWDGL 1666 LSPILNTGPP1676 YCDPNLPNSN1686 GTRGDCGSPA1696 VGIIFFTTYI1706 IISFLIMVNM 1716 YIAVILENFN1726 VA
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SER341
3.722
PHE342
3.978
ALA343
4.152
ASN390
4.613
LEU393
3.340
THR397
3.590
GLU401
3.224
VAL676
4.483
THR679
3.671
ILE680
4.320
VAL763
4.569
LEU766
3.435
SER769
3.583
TRP770
3.436
PRO771
4.165
PHE885
4.150
ILE886
3.760
LEU889
3.713
LEU890
4.837
PHE1214
4.086
THR1215
3.645
ALA1217
3.650
TRP1220
3.541
LEU1224
4.496
LEU1286
4.586
ILE1290
3.419
LEU1293
4.284
VAL1414
3.489
ILE1418
3.182
ASN1422
4.675
ILE1491
4.213
MET1494
3.696
VAL1495
3.479
THR1497
4.099
LYS1504
4.111
PHE1710
4.066
MET1713
2.666
VAL1714
3.266
TYR1717
3.069
ILE1718
3.596
ILE1721
2.629
LEU1722
4.900
PHE1725
3.736
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Protein Name | Pfam ID | Percentage of Identity (%) | E value |
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| Sodium/hydrogen exchanger 11 (SLC9C2) | 27.273 (36/132) | 9.98E-05 |
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Interaction between L1 and Ankyrins | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
| REF 2 | URL: 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 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071810. | |||||
| REF 4 | URL: 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 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040074. | |||||
| REF 6 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
| REF 7 | URL: 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 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 078601. | |||||
| REF 9 | 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 10 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 11 | ClinicalTrials.gov (NCT01327612) Open Label Extension Study of Conatumumab and AMG 479. U.S. National Institutes of Health. | |||||
| REF 12 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 13 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 14 | URL: 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 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017745) | |||||
| REF 16 | 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 17 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 18 | Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian senso... J Biol Chem. 2004 Jun 11;279(24):25774-82. | |||||
| REF 19 | 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 20 | Pathobiology of visceral pain: molecular mechanisms and therapeutic implications. II. Genetic approaches to pain therapy. Am J Physiol Gastrointest Liver Physiol. 2000 Apr;278(4):G507-12. | |||||
| REF 21 | Oral Administration of PF-01247324, a Subtype-Selective Nav1.8 Blocker, Reverses Cerebellar Deficits in a Mouse Model of Multiple Sclerosis. PLoS One. 2015; 10(3): e0119067. | |||||
| REF 22 | 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. | |||||
| REF 23 | Lidocaine reduces the transition to slow inactivation in Na(v)1.7 voltage-gated sodium channels.Br J Pharmacol.2011 Sep;164(2b):719-30. | |||||
| REF 24 | Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. J Med Chem. 2009 May 14;52(9):2694-707. | |||||
| REF 25 | Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. | |||||
| REF 26 | Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. | |||||
| REF 27 | Sensory neuron voltage-gated sodium channels as analgesic drug targets. Curr Opin Neurobiol. 2008 Aug;18(4):383-8. | |||||
| REF 28 | The poison Dart frog's batrachotoxin modulates Nav1.8. FEBS Lett. 2004 Nov 5;577(1-2):245-8. | |||||
| REF 29 | URL: 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). | |||||
| REF 30 | Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52. | |||||
| REF 31 | Novel steroidal saponins, Sch 725737 and Sch 725739, from a marine starfish, Novodinia antillensis. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5543-7. | |||||
| REF 32 | A comparison of the effects of veratridine on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels in isolated rat dorsal root ganglio... Pflugers Arch. 2008 Feb;455(5):929-38. | |||||
| REF 33 | Structural basis for high-voltage activation and subtype-specific inhibition of human Na(v)1.8. Proc Natl Acad Sci U S A. 2022 Jul 26;119(30):e2208211119. | |||||
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