Roles > voltage-gated sodium channel blocker
Page last updated: 2024-08-05 15:38:52

voltage-gated sodium channel blocker

Any sodium channel blocker that interferes with the activity of voltage-gated sodium channels.

ChEBI ID: 38634

Members (4)

MemberDefinitionClass
capsaicincapsaicin
indoxacarbindoxacarb
lanperisoneA 2-methyl-3-(pyrrolidin-1-yl)-1-[4-(trifluoromethyl)phenyl]propan-1-one in which the methyl group at position 2 adopts R-configuration. It is a muscle relaxant and induces ferroptosis in cancer cells.lanperisone
tetrodotoxinA quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.tetrodotoxin

Research

Studies (23,585)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19905,607 (23.77)18.7374
1990's6,362 (26.97)18.2507
2000's6,080 (25.78)29.6817
2010's4,417 (18.73)24.3611
2020's1,119 (4.74)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials675 (2.76%)5.53%
Reviews1,007 (4.12%)6.00%
Case Studies189 (0.77%)4.05%
Observational16 (0.07%)0.25%
Other22,552 (92.28%)84.16%

Protein Targets (84)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency31.622811
67.9K proteinVaccinia virusPotency39.810711
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency21.645215
AR proteinHomo sapiens (human)Potency27.4601920
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.756911
Cellular tumor antigen p53Homo sapiens (human)Potency46.930522
Chain A, HADH2 proteinHomo sapiens (human)Potency35.716822
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency7.943311
Chain B, HADH2 proteinHomo sapiens (human)Potency35.716822
chromobox protein homolog 1Homo sapiens (human)Potency100.000011
cytochrome P450 2D6Homo sapiens (human)Potency2.187611
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency2.511922
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency16.013614
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.125111
estrogen nuclear receptor alphaHomo sapiens (human)Potency35.8668918
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.851122
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.6692611
farnesoid X nuclear receptorHomo sapiens (human)Potency35.825733
GABA theta subunitRattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency2.511911
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency2.511911
GLI family zinc finger 3Homo sapiens (human)Potency6.240123
GLS proteinHomo sapiens (human)Potency8.912511
glucocerebrosidaseHomo sapiens (human)Potency17.782811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency32.580233
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency42.526713
heat shock protein beta-1Homo sapiens (human)Potency30.588922
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency2.818411
lamin isoform A-delta10Homo sapiens (human)Potency35.481311
Microtubule-associated protein tauHomo sapiens (human)Potency24.702822
mitogen-activated protein kinase 1Homo sapiens (human)Potency31.622811
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.213549
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency29.870011
Nuclear receptor ROR-gammaHomo sapiens (human)Potency33.491511
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.481311
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency31.463036
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency9.074311
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency39.711844
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency21.636722
phosphopantetheinyl transferaseBacillus subtilisPotency89.125111
pregnane X nuclear receptorHomo sapiens (human)Potency25.333525
progesterone receptorHomo sapiens (human)Potency37.203423
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.806023
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency6.994324
retinoid X nuclear receptor alphaHomo sapiens (human)Potency17.308724
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency44.668411
survival motor neuron protein isoform dHomo sapiens (human)Potency22.387211
TDP1 proteinHomo sapiens (human)Potency23.132026
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency25.933728
thyroid stimulating hormone receptorHomo sapiens (human)Potency23.710111
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency0.043333
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency18.846711
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency32.642934
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency42.526713

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseHomo sapiens (human)IC50200.000011
Bile salt export pumpHomo sapiens (human)IC5010.000011
Cannabinoid receptor 1Homo sapiens (human)Ki8.900034
Cannabinoid receptor 2 Homo sapiens (human)Ki10.000023
Corticotropin-releasing factor receptor 2Homo sapiens (human)Ki10.000011
Cytochrome P450 1A2Homo sapiens (human)IC503.000011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC500.600033
NADH-ubiquinone oxidoreductase chain 1Bos taurus (cattle)IC5052.480811
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC5056.000011
Potassium voltage-gated channel subfamily A member 1Homo sapiens (human)IC5029.000011
Prostaglandin G/H synthase 1Homo sapiens (human)IC502.675522
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC500.018611
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC500.008022
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)IC500.019011
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Ki1.186544
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)Ki1.779544

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
D(2) dopamine receptorRattus norvegicus (Norway rat)EC500.300011
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)EC501.84631718
Transient receptor potential cation channel subfamily V member 1Rattus norvegicus (Norway rat)EC500.409489
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)EC500.246045
Transient receptor potential cation channel subfamily V member 4Rattus norvegicus (Norway rat)EC500.246045

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Activity0.010011