Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T35135
|
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| Former ID |
TTDS00156
|
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| Target Name |
Voltage-gated sodium channel
|
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| Gene Name |
SCN11A
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| Synonyms |
Voltage-sensitive sodium channel; SCN11A
|
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| Target Type |
Successful
|
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| Disease | Atrial fibrillation; Pain [ICD9: 338, 427.31,780; ICD10: I48, R52, G89] | ||||
| Anesthesia [ICD9: 338; ICD10: R20.0] | |||||
| Amyotrophic lateral sclerosis [ICD9: 335.2; ICD10: G12.2] | |||||
| Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
| Epilepsy; Bipolar disorder [ICD9: 296, 345; ICD10: F31, G40] | |||||
| Epilepsy [ICD10: G40] | |||||
| Multiple scierosis [ICD9: 340; ICD10: G35] | |||||
| Muscle spasm [ICD10: M62.838] | |||||
| Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
| BioChemical Class |
Sodium channel
|
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| Target Validation |
T35135
|
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| UniProt ID | |||||
| Sequence |
MDDRCYPVIFPDERNFRPFTSDSLAAIEKRIAIQKEKKKSKDQTGEVPQPRPQLDLKASR
KLPKLYGDIPRELIGKPLEDLDPFYRNHKTFMVLNRKRTIYRFSAKHALFIFGPFNSIRS LAIRVSVHSLFSMFIIGTVIINCVFMATGPAKNSNSNNTDIAECVFTGIYIFEALIKILA RGFILDEFSFLRDPWNWLDSIVIGIAIVSYIPGITIKLLPLRTFRVFRALKAISVVSRLK VIVGALLRSVKKLVNVIILTFFCLSIFALVGQQLFMGSLNLKCISRDCKNISNPEAYDHC FEKKENSPEFKMCGIWMGNSACSIQYECKHTKINPDYNYTNFDNFGWSFLAMFRLMTQDS WEKLYQQTLRTTGLYSVFFFIVVIFLGSFYLINLTLAVVTMAYEEQNKNVAAEIEAKEKM FQEAQQLLKEEKEALVAMGIDRSSLTSLETSYFTPKKRKLFGNKKRKSFFLRESGKDQPP GSDSDEDCQKKPQLLEQTKRLSQNLSLDHFDEHGDPLQRQRALSAVSILTITMKEQEKSQ EPCLPCGENLASKYLVWNCCPQWLCVKKVLRTVMTDPFTELAITICIIINTVFLAMEHHK MEASFEKMLNIGNLVFTSIFIAEMCLKIIALDPYHYFRRGWNIFDSIVALLSFADVMNCV LQKRSWPFLRSFRVLRVFKLAKSWPTLNTLIKIIGNSVGALGSLTVVLVIVIFIFSVVGM QLFGRSFNSQKSPKLCNPTGPTVSCLRHWHMGDFWHSFLVVFRILCGEWIENMWECMQEA NASSSLCVIVFILITVIGKLVVLNLFIALLLNSFSNEERNGNLEGEARKTKVQLALDRFR RAFCFVRHTLEHFCHKWCRKQNLPQQKEVAGGCAAQSKDIIPLVMEMKRGSETQEELGIL TSVPKTLGVRHDWTWLAPLAEEEDDVEFSGEDNAQRITQPEPEQQAYELHQENKKPTSQR VQSVEIDMFSEDEPHLTIQDPRKKSDVTSILSECSTIDLQDGFGWLPEMVPKKQPERCLP KGFGCCFPCCSVDKRKPPWVIWWNLRKTCYQIVKHSWFESFIIFVILLSSGALIFEDVHL ENQPKIQELLNCTDIIFTHIFILEMVLKWVAFGFGKYFTSAWCCLDFIIVIVSVTTLINL MELKSFRTLRALRPLRALSQFEGMKVVVNALIGAIPAILNVLLVCLIFWLVFCILGVYFF SGKFGKCINGTDSVINYTIITNKSQCESGNFSWINQKVNFDNVGNAYLALLQVATFKGWM DIIYAAVDSTEKEQQPEFESNSLGYIYFVVFIIFGSFFTLNLFIGVIIDNFNQQQKKLGG QDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKCQGLVFDIVTSQIFDIIIISLIILNM ISMMAESYNQPKAMKSILDHLNWVFVVIFTLECLIKIFALRQYYFTNGWNLFDCVVVLLS IVSTMISTLENQEHIPFPPTLFRIVRLARIGRILRLVRAARGIRTLLFALMMSLPSLFNI GLLLFLIMFIYAILGMNWFSKVNPESGIDDIFNFKTFASSMLCLFQISTSAGWDSLLSPM LRSKESCNSSSENCHLPGIATSYFVSYIIISFLIVVNMYIAVILENFNTATEESEDPLGE DDFDIFYEVWEKFDPEATQFIKYSALSDFADALPEPLRVAKPNKYQFLVMDLPMVSEDRL HCMDILFAFTARVLGGSDGLDSMKAMMEEKFMEANPLKKLYEPIVTTTKRKEEERGAAII QKAFRKYMMKVTKGDQGDQNDLENGPHSPLQTLCNGDLSSFGVAKGKVHCD |
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| Drugs and Mode of Action | |||||
| Drug(s) | Lamotrigine | Drug Info | Approved | Epilepsy; Bipolar disorder | [1], [2] |
| Lidocaine | Drug Info | Approved | Anesthesia | [3], [4] | |
| Oxcarbazepine | Drug Info | Approved | Epilepsy | [1], [5] | |
| Riluzole | Drug Info | Approved | Amyotrophic lateral sclerosis | [6], [7] | |
| Tolperisone | Drug Info | Approved | Muscle spasm | [8] | |
| HP-184 | Drug Info | Phase 2 | Multiple scierosis | [6] | |
| Lidocaine | Drug Info | Phase 2 | Dysmenorrhea | [9] | |
| QX-314 | Drug Info | Terminated | Pain | [10], [11] | |
| Blocker | HP-184 | Drug Info | [6] | ||
| Ia Quinidine | Drug Info | [12] | |||
| Ic Flecainide | Drug Info | [12] | |||
| Lamotrigine | Drug Info | [13] | |||
| Lidocaine | Drug Info | [14], [15] | |||
| Oxcarbazepine | Drug Info | [16], [17] | |||
| QX-314 | Drug Info | [18] | |||
| Riluzole | Drug Info | [19] | |||
| SB-221420-A | Drug Info | [20] | |||
| Modulator | Tolperisone | Drug Info | [21], [8] | ||
| References | |||||
| REF 1 | Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54. | ||||
| REF 2 | (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: 2622). | ||||
| REF 3 | An absorbable local anesthetic matrix provides several days of functional sciatic nerve blockade. Anesth Analg. 2009 Mar;108(3):1027-33. | ||||
| 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: 2623). | ||||
| REF 5 | (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: 7254). | ||||
| REF 6 | Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80. | ||||
| REF 7 | (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: 2326). | ||||
| REF 8 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 9 | ClinicalTrials.gov (NCT00651313) Efficacy and Safety Study of Lidocaine Vaginal Gel for Recurrent Dysmenorrhea (Painful Periods). U.S. National Institutes of Health. | ||||
| 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: 2405). | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008413) | ||||
| REF 12 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | ||||
| REF 13 | The effects of lamotrigine on the acquisition and expression of morphine-induced place preference in mice. Pak J Biol Sci. 2009 Jan 1;12(1):33-9. | ||||
| REF 14 | Mechanisms of analgesia of intravenous lidocaine. Rev Bras Anestesiol. 2008 May-Jun;58(3):280-6. | ||||
| REF 15 | Lidocaine inhibits epithelial chemokine secretion via inhibition of nuclear factor kappaB activation. Immunobiology. 2009 Jun 24. | ||||
| REF 16 | Antiepileptic drugs in non-epilepsy disorders: relations between mechanisms of action and clinical efficacy. CNS Drugs. 2008;22(1):27-47. | ||||
| REF 17 | Debate: Does genetic information in humans help us treat patients? PRO--genetic information in humans helps us treat patients. CON--genetic information does not help at all. Epilepsia. 2008 Dec;49 Suppl 9:13-24. | ||||
| REF 18 | Voltage-gated sodium channel blockers for the treatment of chronic pain. Curr Top Med Chem. 2009;9(4):362-76. | ||||
| REF 19 | Secondary injury mechanisms of spinal cord trauma: a novel therapeutic approach for the management of secondary pathophysiology with the sodium channel blocker riluzole. Prog Brain Res. 2002;137:177-90. | ||||
| REF 20 | Recent updates of N-type calcium channel blockers with therapeutic potential for neuropathic pain and stroke. Curr Top Med Chem. 2009;9(4):377-95. | ||||
| REF 21 | 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. | ||||
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