DGIdb - SCN10A Gene Record

SCN10A 6336 Druggable Genome

Alternate Names:

6336
SODIUM VOLTAGE-GATED CHANNEL ALPHA SUBUNIT 10
SCN10A
FEPS2
Nav1.8
PN3
SNS
hPN3
604427
10582
ENSG00000185313
OTTHUMG00000048245
Q9Y5Y9
SCNAA_HUMAN
TTDS00514
SODIUM CHANNEL PROTEIN TYPE 10 SUBUNIT ALPHA
VOLTAGE-GATED SODIUM CHANNEL SUBUNIT ALPHA NAV1.8
SODIUM CHANNEL PROTEIN TYPE X SUBUNIT ALPHA
PERIPHERAL NERVE SODIUM CHANNEL 3
TTDS00157
VOLTAGE-GATED SODIUM CHANNEL NAV1.8
TRANSIENT TETRODOTOXIN-RESISTANT NA+ CURRENT
TTX-R SODIUM CHANNEL
TTX-R/NAV1.8
585
Na<sub>v</sub>1.8
NP_006505
NM_006514
sodium channel, voltage-gated, type X, alpha subunit
SODIUM CHANNEL PROTEIN TYPE X ALPHA SUBUNIT (VOLTAGE-GATED SODIUM CHANNEL ALPHA SUBUNIT NAV1.8) (PERIPHERAL NERVE SODIUM CHANNEL 3) (HPN3). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5Y9]
BE0000177
PA35000
Voltage-gated sodium channel alpha Nav1.8
T43739

Gene Info:

GuideToPharmacology Gene Category Name	Voltage-gated sodium channels
GuideToPharmacology Gene Category ID	82
GuideToPharmacology Gene Type	vgic
Target Main Class	Transporters
Transmembrane Helix Count	23
Target Subclass	Voltage_gated_ion_channels
Target Subclass	SodiumChannels
Target Subclass	Channels
Target Class	Transporters
Target Subclass	TC:1.A.1.10
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	Ion_trans_dom
Interpro Acc	IPR005821
Uniprot Status	Swiss-Prot
Interpro Name	Ion transport domain
Interpro Type	Domain
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	ION CHANNEL
Initial Gene Query	Nav1.8
Counted Citations from 1950-2000	298
Gene Biotype	PROTEIN_CODING

(10 More Sources)

Gene Categories: Category Details

TRANSPORTER
ION CHANNEL
DRUGGABLE GENOME

Publications:

Roghani et al., Evaluating the efficacy of commonly used topical anesthetics., Pediatr Dent
Tella et al., 1998, Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine., Pharmacol. Biochem. Behav.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Sheets et al., 2010, Sodium channel molecular conformations and antiarrhythmic drug affinity., Trends Cardiovasc. Med.
Hung et al., 2009, Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats., Neurosci. Lett.
Ahern et al., 2008, Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels., Circ. Res.
Hanck et al., 2009, Using lidocaine and benzocaine to link sodium channel molecular conformations to state-dependent antiarrhythmic drug affinity., Circ. Res.
Lipkind et al., 2005, Molecular modeling of local anesthetic drug binding by voltage-gated sodium channels., Mol. Pharmacol.
Liu et al., 2000, The effects of ropivacaine on sodium currents in dorsal horn neurons of neonatal rats., Anesth. Analg.
Louro et al., 1998, Carboxyl groups at the membrane interface as molecular targets for local anesthetics., Biophys. Chem.
Ryan et al., 1996, Structural effects of neutral and anionic lipids on the nicotinic acetylcholine receptor. An infrared difference spectroscopy study., J. Biol. Chem.
Muroi et al., 2009, Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel., J. Gen. Physiol.
Ekberg et al., 2006, muO-conotoxin MrVIB selectively blocks Nav1.8 sensory neuron specific sodium channels and chronic pain behavior without motor deficits., Proc. Natl. Acad. Sci. U.S.A.
Karoly et al., 2010, Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study., PLoS Comput. Biol.
Chevrier P et al., 2004, Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine., Br J Pharmacol
Leffler et al., 2010, Block of sensory neuronal Na+ channels by the secreolytic ambroxol is associated with an interaction with local anesthetic binding sites., Eur. J. Pharmacol.
He YJ et al., 2016, Carboplatin/taxane-induced gastrointestinal toxicity: a pharmacogenomics study on the SCOTROC1 trial., Pharmacogenomics J
Wong et al., 1993, On the mechanisms of potentiation of local anesthetics by bicarbonate buffer: drug structure-activity studies on isolated peripheral nerve., Anesth. Analg.
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Ueta et al., In vitro antagonism of recombinant ligand-gated ion-channel receptors by stereospecific enantiomers of bupivacaine., Reg Anesth Pain Med
Vladimirov et al., 2000, Potency of bupivacaine stereoisomers tested in vitro and in vivo: biochemical, electrophysiological, and neurobehavioral studies., Anesthesiology
Bräu et al., 2000, Block of neuronal tetrodotoxin-resistant Na+ currents by stereoisomers of piperidine local anesthetics., Anesth. Analg.
Katalymov, 1995, [The effect of inhibitors of sodium permeability (novocaine and tetrodotoxin) on the trace depolarization of myelinated nerve fibers]., Fiziol Zh Im I M Sechenova
Bräu et al., 1998, Fundamental properties of local anesthetics: half-maximal blocking concentrations for tonic block of Na+ and K+ channels in peripheral nerve., Anesth. Analg.
Creveling et al., 1990, Procaine isothiocyanate: an irreversible inhibitor of the specific binding of [3H]batrachotoxinin-A benzoate to sodium channels., Neurochem. Res.
Pubill et al., 1999, Assessment of the adrenergic effects of orphenadrine in rat vas deferens., J. Pharm. Pharmacol.

BUPIVACAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Durect

Trial Name DUR-843,Eladur, Transdur-Bupivacaine

Trial Name DepoBupivacaine, bupivacaine,Exparel

Publications:

Sheets et al., 2010, Sodium channel molecular conformations and antiarrhythmic drug affinity., Trends Cardiovasc. Med.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

LIDOCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Trial Name ALGRX 3268,Zingo

Novel drug target Established target

Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

Publications:

Muroi et al., 2009, Local anesthetics disrupt energetic coupling between the voltage-sensing segments of a sodium channel., J. Gen. Physiol.

Ekberg et al., 2006, muO-conotoxin MrVIB selectively blocks Nav1.8 sensory neuron specific sodium channels and chronic pain behavior without motor deficits., Proc. Natl. Acad. Sci. U.S.A.

Karoly et al., 2010, Fast- or slow-inactivated state preference of Na+ channel inhibitors: a simulation and experimental study., PLoS Comput. Biol.

ARTICAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
FOSPHENYTOIN SODIUM SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
HEXYLCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
TETRACAINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
ROPIVACAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
ORPHENADRINE CITRATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
RUFINAMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
DIBUCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Publications:
QUINIDINE GLUCONATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
ZONISAMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
MEPHENYTOIN SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
ORPHENADRINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
DYCLONINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
LAMOTRIGINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
MERETHOXYLLINE PROCAINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
PROPOXYCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PF-04531083 SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Direct Interaction yes

Publications:
RALFINAMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
ETHOTOIN SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
PHENYTOIN SODIUM SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
MEXILETINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
DISOPYRAMIDE PHOSPHATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
RILUZOLE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
DRONEDARONE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
NERISPIRDINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
ESLICARBAZEPINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
TOPIRAMATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
TOCAINIDE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PRILOCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
EVENAMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PRILOCAINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PROPAFENONE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PHENAZOPYRIDINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
OXCARBAZEPINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PROPARACAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
CARBAMAZEPINE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
MEPIVACAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
LIDOCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
CHLOROPROCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
ESLICARBAZEPINE ACETATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
DSP-2230 SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Direct Interaction yes

Publications:
AFACIFENACIN SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Direct Interaction yes

Publications:
ETIDOCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:
QUINIDINE POLYGALACTURONATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
INDECAINIDE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PROCAINAMIDE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
BENOXINATE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
QUINIDINE SULFATE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PHENACEMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PRIMIDONE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PHENYTOIN SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
IRAMPANEL SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
MORICIZINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
NKTR-171 SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
PROCAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:
TETRACAINE HYDROCHLORIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:

DYCLONINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Roghani et al., Evaluating the efficacy of commonly used topical anesthetics., Pediatr Dent

Tella et al., 1998, Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine., Pharmacol. Biochem. Behav.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

PROPARACAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Tella et al., 1998, Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine., Pharmacol. Biochem. Behav.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

BENOXINATE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Hung et al., 2009, Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats., Neurosci. Lett.

BENZOCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Ahern et al., 2008, Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels., Circ. Res.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

ROPIVACAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name ropivacaine HCl,Naropin

Novel drug target Established target

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Liu et al., 2000, The effects of ropivacaine on sodium currents in dorsal horn neurons of neonatal rats., Anesth. Analg.

DIBUCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Louro et al., 1998, Carboxyl groups at the membrane interface as molecular targets for local anesthetics., Biophys. Chem.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

HEXYLCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Chevrier P et al., 2004, Differential modulation of Nav1.7 and Nav1.8 peripheral nerve sodium channels by the local anesthetic lidocaine., Br J Pharmacol

MEPIVACAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name APF 112, mepivacaine sustained-release

Novel drug target Established target

Publications:

Leffler et al., 2010, Block of sensory neuronal Na+ channels by the secreolytic ambroxol is associated with an interaction with local anesthetic binding sites., Eur. J. Pharmacol.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

CHLOROPROCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Wong et al., 1993, On the mechanisms of potentiation of local anesthetics by bicarbonate buffer: drug structure-activity studies on isolated peripheral nerve., Anesth. Analg.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

COCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
ERLOSAMIDE SCN10A

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Publications:

Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.

LEVOBUPIVACAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Ueta et al., In vitro antagonism of recombinant ligand-gated ion-channel receptors by stereospecific enantiomers of bupivacaine., Reg Anesth Pain Med

Vladimirov et al., 2000, Potency of bupivacaine stereoisomers tested in vitro and in vivo: biochemical, electrophysiological, and neurobehavioral studies., Anesthesiology

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

PROCAINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Katalymov, 1995, [The effect of inhibitors of sodium permeability (novocaine and tetrodotoxin) on the trace depolarization of myelinated nerve fibers]., Fiziol Zh Im I M Sechenova

Bräu et al., 1998, Fundamental properties of local anesthetics: half-maximal blocking concentrations for tonic block of Na+ and K+ channels in peripheral nerve., Anesth. Analg.

Creveling et al., 1990, Procaine isothiocyanate: an irreversible inhibitor of the specific binding of [3H]batrachotoxinin-A benzoate to sodium channels., Neurochem. Res.

ORPHENADRINE SCN10A

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

Pubill et al., 1999, Assessment of the adrenergic effects of orphenadrine in rat vas deferens., J. Pharm. Pharmacol.
TETRODOTOXIN SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name tetrodotoxin,Tectin, Tetrodin

Novel drug target Established target

Publications:
CARBOPLATIN SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

He YJ et al., 2016, Carboplatin/taxane-induced gastrointestinal toxicity: a pharmacogenomics study on the SCOTROC1 trial., Pharmacogenomics J
chembl:CHEMBL250699 SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL448556 SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
TIAPRIDE SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL421719 SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CONATUMUMAB SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
VERATRIDINE SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
RILPIVIRINE SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1162029 SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1162028 SCN10A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000185313
- Version: 101_38
Alternate Names:

SCN10A Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: Q9Y5Y9
- Version: 01-August-2011
Alternate Names:

6336 Entrez Gene Id

SCNAA_HUMAN Uniprot Id

SCN10A Gene Symbol

Gene Info:

Target Main Class Transporters

Transmembrane Helix Count 23

Target Subclass Voltage_gated_ion_channels

Publications:
GuideToPharmacologyGenes: 585
- Version: 4-March-2015
Alternate Names:

sodium channel, voltage-gated, type X, alpha subunit HUGO Gene Name

10582 HUGO Gene ID

SCN10A Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name Voltage-gated sodium channels

GuideToPharmacology Gene Category ID 82

GuideToPharmacology Gene Type vgic

Gene Categories:

TRANSPORTER, ION CHANNEL

Publications:
TdgClinicalTrial: Q9Y5Y9
- Version: January-2014
Alternate Names:

SCN10A Gene Symbol

Gene Info:

Target Class Transporters

Target Subclass TC:1.A.1.10

Publications:
HopkinsGroom: Q9Y5Y9
- Version: 11-September-2012
Alternate Names:

SCNAA_HUMAN Uniprot Id

SODIUM CHANNEL PROTEIN TYPE 10 SUBUNIT ALPHA Uniprot Protein Name

SCN10A Uniprot Gene Name

Gene Info:

Interpro Short Name Ion_trans_dom

Interpro Acc IPR005821

Uniprot Status Swiss-Prot

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:

RussLampel: ENSG00000185313

Version: 26-July-2011

Alternate Names:

SODIUM CHANNEL PROTEIN TYPE X ALPHA SUBUNIT (VOLTAGE-GATED SODIUM CHANNEL ALPHA SUBUNIT NAV1.8) (PERIPHERAL NERVE SODIUM CHANNEL 3) (HPN3). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5Y9] Description

SCN10A Display Id

ENSG00000185313 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

BaderLabGenes: SCN10A
- Version: February-2014
Alternate Names:

6336 Entrez Gene ID

Gene Info:

Initial Gene Query Nav1.8

Counted Citations from 1950-2000 298

Gene Categories:

ION CHANNEL

Publications:
PharmGKB: SCN10A
- Version: 18-August-2020
Alternate Names:

PA35000 PharmGKB ID

Gene Info:

Publications:

He YJ et al., 2016, Carboplatin/taxane-induced gastrointestinal toxicity: a pharmacogenomics study on the SCOTROC1 trial., Pharmacogenomics J
TTD: Voltage-gated sodium channel alpha Nav1.8
- Version: 2020.06.01
Alternate Names:

SCN10A TTD Gene Abbreviation

T43739 TTD Target ID

Gene Info:

Publications:

Shields SD et al., 2015, Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis., PLoS One

DrugBank: BE0000177

Version: 5.1.7

Alternate Names:

SCN10A DrugBank Gene Name

Q9Y5Y9 UniProt Accession

6336 Entrez Gene Id

Gene Info:

Publications:

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

Liu et al., 2000, The effects of ropivacaine on sodium currents in dorsal horn neurons of neonatal rats., Anesth. Analg.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

HingoraniCasas: ENSG00000185313
- Version: 31-May-2017
Alternate Names:

ENSG00000185313 Gene Symbol

SCN10A Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: SCN10A
- Version: chembl_23
Alternate Names:

SCN10A GENE_SYMBOL

Sodium channel protein type 10 subunit alpha UNIPROT

Peripheral nerve sodium channel 3 UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000185313
- Version: 20-July-2020
Alternate Names:

Na<sub>v</sub>1.8 GuideToPharmacology Name

Q9Y5Y9 UniProtKB ID

Gene Info:

Publications:
Pharos: SCN10A
- Version: 03-September-2020
Alternate Names:

Sodium channel protein type 10 subunit alpha Gene Name

Q9Y5Y9 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Trial Name	Durect
Trial Name	DUR-843,Eladur, Transdur-Bupivacaine
Trial Name	DepoBupivacaine, bupivacaine,Exparel

Trial Name	ALGRX 3268,Zingo
Novel drug target	Established target
Trial Name	lidocaine hydrochloride, piroxicam, AK1015,Akten

Mechanism of Interaction	Sodium channel alpha subunit blocker
Direct Interaction	yes

Trial Name	ropivacaine HCl,Naropin
Novel drug target	Established target

Trial Name	APF 112, mepivacaine sustained-release
Novel drug target	Established target

Trial Name	tetrodotoxin,Tectin, Tetrodin
Novel drug target	Established target

sodium channel, voltage-gated, type X, alpha subunit	HUGO Gene Name
10582	HUGO Gene ID
SCN10A	Gene Symbol

SCNAA_HUMAN	Uniprot Id
SODIUM CHANNEL PROTEIN TYPE 10 SUBUNIT ALPHA	Uniprot Protein Name
SCN10A	Uniprot Gene Name

SODIUM CHANNEL PROTEIN TYPE X ALPHA SUBUNIT (VOLTAGE-GATED SODIUM CHANNEL ALPHA SUBUNIT NAV1.8) (PERIPHERAL NERVE SODIUM CHANNEL 3) (HPN3). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5Y9]	Description
SCN10A	Display Id
ENSG00000185313	Ensembl Gene Id

SCN10A	DrugBank Gene Name
Q9Y5Y9	UniProt Accession
6336	Entrez Gene Id

SCN10A	GENE_SYMBOL
Sodium channel protein type 10 subunit alpha	UNIPROT
Peripheral nerve sodium channel 3	UNIPROT

Sodium channel protein type 10 subunit alpha	Gene Name
Q9Y5Y9	UniProt ID

SCN10A Gene Record

SCN10A 6336 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Durect Trial Name DUR-843,Eladur, Transdur-Bupivacaine Trial Name DepoBupivacaine, bupivacaine,Exparel

Interaction Types & Directionality: inhibitor (inhibitory) blocker (inhibitory)

Interaction Info: Trial Name ALGRX 3268,Zingo Novel drug target Established target Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel protein type X alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sodium channel alpha subunit blocker

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel alpha subunit blocker Direct Interaction yes

Publications:

Interaction Types & Directionality: blocker (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Durect

Trial Name DUR-843,Eladur, Transdur-Bupivacaine

Trial Name DepoBupivacaine, bupivacaine,Exparel

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Trial Name ALGRX 3268,Zingo

Novel drug target Established target

Trial Name lidocaine hydrochloride, piroxicam, AK1015,Akten

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type X alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sodium channel alpha subunit blocker

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel alpha subunit blocker

Direct Interaction yes