Page last updated: 2024-11-13

saxitoxin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

Saxitoxin: A compound that contains a reduced purine ring system but is not biosynthetically related to the purine alkaloids. It is a poison found in certain edible mollusks at certain times; elaborated by GONYAULAX and consumed by mollusks, fishes, etc. without ill effects. It is neurotoxic and causes RESPIRATORY PARALYSIS and other effects in MAMMALS, known as paralytic SHELLFISH poisoning. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

saxitoxin : An alkaloid isolated from the marine dinoflagellates and cyanobacteria that causes paralytic shellfish poisoning. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID56947150
CHEMBL ID501134
CHEBI ID34970
SCHEMBL ID49687
SCHEMBL ID13028580
SCHEMBL ID22829661
MeSH IDM0019455

Synonyms (34)

Synonym
gonyaulax catenella poison
1h,10h-pyrrolo(1,2-c)purine-10,10-diol, 2,6-diamino-4-(((amino-carbonyl)oxy)methyl)-3a,4,8,9-tetrahydro-, (3as-(3a-alpha,4-alpha,10ar*))
mytilus californianus poison
saxitoxin hydrate
saxidomus giganteus poison
gtpl2625
saxitoxin
35523-89-8
saxitoxin (8ci)
[(3as,4r,10as)-2,6-diamino-10,10-dihydroxy-3a,4,8,9-tetrahydro-3h-pyrrolo[1,2-c]purin-4-yl]methyl carbamate
1h,10h-pyrrolo(1,2-c)purine-10,10-diol, 2,6-diamino-4-(((aminocarbonyl)oxy)methyl)-3a,4,8,9-tetrahydro-, (3as-(3aalpha,4alpha,10ar*))-
(+)-saxitoxin
chebi:34970 ,
CHEMBL501134
1h,10h-pyrrolo(1,2-c)purine-10,10-diol, 2,6-diamino-4-(((aminocarbonyl)oxy)methyl)-3a,4,8,9-tetrahydro-, labeled with tritium, (3as-(3aalpha,4alpha,10ar*))-
saxitoxin-3h
saxitoxin-t
unii-q0638e899b
q0638e899b ,
1h,10h-pyrrolo(1,2-c)purine-10,10-diol, 2,6-diamino-4-(((aminocarbonyl)oxy)methyl)-3a,4,8,9-tetrahydro-, (3as,4r,10as)-
S-1900
saxitoxin [mi]
saxitoxin (hydrate)
SCHEMBL49687
SCHEMBL13028580
[(3as,4r,10as)-10,10-dihydroxy-2,6-diiminooctahydro-1h,8h-pyrrolo[1,2-c]purin-4-yl]methyl carbamate
DTXSID3074313
[(r,7as,7bs)-2-amino-7,7-dihydroxy--imino-h,h,h,1h,5h,6h,7h,7bh-pyrrolo[1,2-c]purin--yl]methyl carbamate
saxitoxin in acetic acid (determination in mussel), bcr(r) certified reference material
bdbm190233
us9174999, table 1, compound 1
Q412694
[(3as,4r,10as)-2,6-diamino-10,10-dihydroxy-3a,4,8,9-tetrahydro-1h-pyrrolo[1,2-c]purin-4-yl]methyl carbamate
SCHEMBL22829661

Research Excerpts

Toxicity

Saxitoxin can cause various toxic effects in aquatic organisms. Toxicity was determined in dinoflagellate cell extracts by different methods: high-performance liquid chromatography (HPLC) and electrophysiological test.

ExcerptReferenceRelevance
" The results indicate that animal cell cultures are useful for studies of general cytotoxins that affect common essential metabolism but cannot be used to detect environmental toxins that cause toxic manifestations by an interference with specific physiological functions of organ systems."( Comparative cytotoxicity of aflatoxin B1 and saxitoxin in cell cultures.
Barter, S; Gabliks, J,
)
0.13
" The shrimp ingested the dinoflagellate cells and an LD50 determination was made."( Toxicity of Gonyaulax tamarensis var. excavata cells to the brine shrimp Artemia salina L.
Betz, JM; Blogoslawski, WJ, 1982
)
0.26
"Farmed mussels were artificially contaminated with a pure culture of an Alexandrium tamarense toxic strain (MOG 835), to assess the effect of initial toxicity on paralytic toxin change during the depuration process."( Influence of initial toxicity and extraction procedure on paralytic toxin changes in the mussel.
Bardouil, M; Bohec, M; Lassus, P; Ledoux, M, 1993
)
0.29
"The toxic dinoflagellate Alexandrium minutum T1 was isolated from southern Taiwan in February 1996, grown under various environmental and nutritional conditions, and then examined for growth, toxicity, and toxin profile."( Influence of environmental and nutritional factors on growth, toxicity, and toxin profile of dinoflagellate Alexandrium minutum.
Hwang, DF; Lu, YH, 2000
)
0.31
" Therefore, in the near future, the proposed biosensor system may be used for monitoring the STX (saxitoxin) produced by a few naturally toxic phytoplankton, and also measuring small amounts of toxin in shellfish."( Application of a channel biosensor for toxicity measurements in cultured Alexandrium tamarense.
Cheun, BS; Han, MS; Lee, HO; Watanabe, E; Yoo, JS, 2000
)
0.31
" Toxicity was determined in dinoflagellate cell extracts by different methods: high-performance liquid chromatography (HPLC); an electrophysiological test called the Electrotest, which measures the inhibition of saxitoxin-sensitive Na(+) channels expressed in a cell line; and a mouse bioassay, which measures the toxic effect on the whole mammal neuromuscular system."( Effect of associated bacteria on the growth and toxicity of Alexandrium catenella.
Espejo, RT; Uribe, P, 2003
)
0.32
" Therefore, populations utilizing high ammonium concentration could be more toxic than those growing on nitrate or urea."( Variability in toxicity of the dinoflagellate Alexandrium tamarense in response to different nitrogen sources and concentrations.
Leong, SC; Murata, A; Nagashima, Y; Taguchi, S, 2004
)
0.32
" The results showed a wide range of responses with strains showing no signs of poisoning and strains producing protracted or slightly protracted toxic effects."( Toxicity of culturable cyanobacteria strains isolated from the Portuguese coast.
Fastner, J; Martins, R; Pereira, P; Vasconcelos, VM; Welker, M, 2005
)
0.33
" asellus extracts, indicating that TTX and its analogs are not the main toxic components of the extracts."( Toxicity and toxin identification in Colomesus asellus, an Amazonian (Brazil) freshwater puffer fish.
Bloch, C; de Freitas, JC; Fernandes, SC; Melo, JA; Oliveira, JS; Rodrigues Pires, O; Schwartz, CA, 2006
)
0.33
" Results of bioassays showed adverse effects including death, paralysis, and reduced population growth rate, generally proportional to the reservoir water concentration."( Biomonitoring of cyanotoxins in two tropical reservoirs by cladoceran toxicity bioassays.
Azevedo, SM; da S Ferrão-Filho, A; de Freitas Magalhães, V; Soares, MC, 2009
)
0.35
"The therapeutic properties of gonyautoxin local infiltration in chronic tension-type headache patients are shown to be safe and effective."( Local infiltration of gonyautoxin is safe and effective in treatment of chronic tension-type headache.
García, C; Lagos, M; Lagos, N; Lattes, K; Pedraza, L; Rodriguez-Navarro, AJ; Venegas, P, 2009
)
0.35
" Our results showed no correlation between toxic phenotype and phylogenetic association in the Australian strains."( Toxicity phenotype does not correlate with phylogeny of Cylindrospermopsis raciborskii strains.
Fuentes-Valdés, JJ; Méndez, MA; Murillo, AA; Soto-Liebe, K; Stucken, K; Vásquez, M, 2009
)
0.35
" To protect human health, seafood harvesting bans are in effect when toxins exceed a safe action level (typically 80 microg STX eq 100 g(-1) tissue)."( Paralytic shellfish poisoning: seafood safety and human health perspectives.
Etheridge, SM, 2010
)
0.36
"Contamination of water bodies by saxitoxin can result in various toxic effects in aquatic organisms."( Investigation of animal and algal bioassays for reliable saxitoxin ecotoxicity and cytotoxicity risk evaluation.
Creppy, EE; Matias, MS; Matias, WG; Melegari, SP; Perreault, F; Pinto, CR; Popovic, R, 2011
)
0.37
" The toxins responsible for this type of poisoning are highly toxic natural compounds produced by dinoflagellates, which bind to voltage-gated Na(+) channels causing the blockade of action potential propagation."( Determination of toxicity equivalent factors for paralytic shellfish toxins by electrophysiological measurements in cultured neurons.
Alonso, E; Botana, AM; Botana, LM; Perez, S; Vale, C; Vieytes, MR, 2011
)
0.37
" The LD50 of the aphantoxin preparation was determined to be 11."( Zebrafish neurotoxicity from aphantoxins--cyanobacterial paralytic shellfish poisons (PSPs) from Aphanizomenon flos-aquae DC-1.
Hu, C; Li, D; Li, G; Liu, Y; Wang, G; Zhang, D, 2013
)
0.39
" Nevertheless, the knowledge regarding metabolism of PSTs and their toxic effects in fish is scarce."( Biotransformation modulation and genotoxicity in white seabream upon exposure to paralytic shellfish toxins produced by Gymnodinium catenatum.
Barata, M; Costa, PR; Guilherme, S; Nicolau, L; Pacheco, M; Pereira, P; Pousão-Ferreira, P; Santos, MA, 2012
)
0.38
" The dissociated cells were plated with medium and different STXs concentrations and the toxic cellular effects such as oxidative stress, neurotoxicity, and genotoxicity and apoptosis process were evaluated."( Saxitoxins induce cytotoxicity, genotoxicity and oxidative stress in teleost neurons in vitro.
Cestari, MM; Costa, MD; da Silva, CA; de Assis, HC; de Morais, EC; Guiloski, IC; Magalhães, VF; Ramsdorf, WA; Ribas, JL; Ribeiro, CA; Trudeau, VL; Zanata, SM, 2014
)
0.4
" This study revealed that NeoSTX is safe in vivo, giving a reliable security margin for its use like a local anesthetic."( Chronic toxicity study of neosaxitoxin in rats.
Candiracci, M; Lobos, N; Lux, S; Miranda, HF; Zepeda, RJ, 2014
)
0.4
" Primary outcome measures were safety and adverse events associated with NeoSTX."( A Phase 1, Dose-escalation, Double-blind, Block-randomized, Controlled Trial of Safety and Efficacy of Neosaxitoxin Alone and in Combination with 0.2% Bupivacaine, with and without Epinephrine, for Cutaneous Anesthesia.
Alexander, ME; Berde, CB; Bilge, A; Boretsky, K; Cornelissen, L; Cravero, J; Donado, C; Kellogg, M; Kim, J; Kurgansky, KE; Lobo, K; McCann, ME; Ortiz, R; Peake, RW; Peyton, J; Zurakowski, D, 2015
)
0.42
"A total of 84 subjects were randomized and completed the two-part trial with no serious adverse events or clinically significant physiologic impairments."( A Phase 1, Dose-escalation, Double-blind, Block-randomized, Controlled Trial of Safety and Efficacy of Neosaxitoxin Alone and in Combination with 0.2% Bupivacaine, with and without Epinephrine, for Cutaneous Anesthesia.
Alexander, ME; Berde, CB; Bilge, A; Boretsky, K; Cornelissen, L; Cravero, J; Donado, C; Kellogg, M; Kim, J; Kurgansky, KE; Lobo, K; McCann, ME; Ortiz, R; Peake, RW; Peyton, J; Zurakowski, D, 2015
)
0.42
"NeoSTX combinations have a tolerable side effect profile and appear promising for prolonged local anesthesia."( A Phase 1, Dose-escalation, Double-blind, Block-randomized, Controlled Trial of Safety and Efficacy of Neosaxitoxin Alone and in Combination with 0.2% Bupivacaine, with and without Epinephrine, for Cutaneous Anesthesia.
Alexander, ME; Berde, CB; Bilge, A; Boretsky, K; Cornelissen, L; Cravero, J; Donado, C; Kellogg, M; Kim, J; Kurgansky, KE; Lobo, K; McCann, ME; Ortiz, R; Peake, RW; Peyton, J; Zurakowski, D, 2015
)
0.42
" P-glycoprotein (P-gp) is a well-known ATP-binding cassette (ABC) transporter that plays a crucial role in the extrusion of toxic substances, decreasing their accumulation and potential intracellular effects in virtue of its broad substrate specificity, its expression in many excretory tissues and its large efflux capacity."( Cytoprotection of lipoic acid against toxicity induced by saxitoxin in hippocampal cell line HT-22 through in silico modeling and in vitro assays.
Cornetet, LR; de Souza Votto, AP; Dos Santos Machado, K; Durruthy, MG; Fagan, SB; Gama, S; Monserrat, JM; Portantiolo, A; Ramos, P; Schmitz, M; Tonel, MZ; Werhli, A; Yunes, JS, 2018
)
0.48
" However, the European Food Safety Authority (EFSA) has established a safety level of 44 µg/kg TTX as the amount of toxin that did not cause adverse effects in humans."( Oral Chronic Toxicity of the Safe Tetrodotoxin Dose Proposed by the European Food Safety Authority and Its Additive Effect with Saxitoxin.
Boente-Juncal, A; Botana, LM; Camiña, M; Otero, P; Rodríguez, I; Rodriguez-Vieytes, M; Vale, C, 2020
)
0.56
" A large gap in our understanding is the genetic variability among natural bloom populations, as both toxic and non-toxic strains have been isolated from the same geographic location."( Bioluminescence and toxicity as driving factors in harmful algal blooms: Ecological functions and genetic variability.
Cusick, KD; Widder, EA, 2020
)
0.56
"Harmful cyanobacterial blooms are increasing and becoming a worldwide concern as many bloom-forming cyanobacterial species can produce toxic metabolites named cyanotoxins."( In Vivo and In Vitro Toxicity Testing of Cyanobacterial Toxins: A Mini-Review.
Lima, ST; Metcalf, JS; Nowruzi, B; Porzani, SJ, 2021
)
0.62
"Saxitoxin and its derivatives, the paralytic shellfish toxins (PSTs), are well known to be toxic to humans, and maximum permitted levels in seafood have been established by regulatory authorities in many countries."( Acute toxicity of decarbamoyl gonyautoxin 1&4 to mice by various routes of administration.
Boundy, MJ; Burger, E; Finch, S; Harwood, DT; Selwood, AI; Tommasi, E; van Ginkel, R; Waugh, C, 2021
)
0.62
" Diatoms dominated the microalgae composition, followed by dinoflagellates, some of which are reported to be potentially toxic and producers of paralytic shellfish toxins."( Evaluation of Paralytic Shellfish Toxins in Marine Oyster Farming and Microalgae in the Atlantic Amazon Evidences Safety but Highlights Potential Risks of Shellfish Poisoning.
Alves, FADS; da Silva Rocha, CC; de Oliveira Lima, M; de Sousa, EB; Faustino, SMM; Martins, MP; Mendes, RA; Schneider, MPC, 2022
)
0.72
" The dependence on animal data to keep humans safe means that it is critical that the toxicity data used is robust and of high quality."( The Effect of Experimental Protocol on the Toxicity of Saxitoxin in Mice.
Boundy, MJ; Finch, SC; Harwood, DT; Webb, NG, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic studies (absorption, distribution and accumulation) reported on Takifugu rubripes, Takifugu pardalis, Takifugu niphobles, Takifugu vermicularis, Takifugu snyderi, etc."( Binding and Pharmacokinetics of the Sodium Channel Blocking Toxins (Saxitoxin and the Tetrodotoxins).
Pratheepa, V; Vasconcelos, V, 2017
)
0.46
" We describe the development and validation of a highly sensitive method for measurement of neosaxitoxin in human plasma using liquid chromatography tandem mass spectrometry (LC-MS/MS) and provide evidence for its use in a human pharmacokinetic study."( Measurement of neosaxitoxin in human plasma using liquid-chromatography tandem mass spectrometry: Proof of concept for a pharmacokinetic application.
Azcue, N; Berde, CB; Hartigan, CE; Kellogg, MD; Peake, RW; Prabhakara, J; Shkreta, A; Zhang, VY, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
" Combined with or covalently coupled to antigens, they act as potent adjuvants."( Preparation of human and murine monoclonal antibodies: antigens combined with or conjugated to lipopeptides constitute potent immunogens for in vitro and in vivo immunizations.
Hoffmann, P; Jimenez-Diaz, M; Jung, G; Kaiser, I; Lenzner, S; Loleit, M; Metzger, J; Stöcklin, S; Tröger, W; Wiesmüller, KH, 1990
)
0.28
" Column switching and two-step gradient elution using HILIC combined with mass spectrometry enabled the simultaneous analysis of the 15 primary STX analogues and their biosynthetic intermediates, arginine, Int-A', and Int-C'2, and the shunt product, Cyclic-C'."( Column switching combined with hydrophilic interaction chromatography-tandem mass spectrometry for the analysis of saxitoxin analogues, and their biosynthetic intermediates in dinoflagellates.
Cho, Y; Konoki, K; Omura, T; Oshima, Y; Tsuchiya, S; Yoshioka, R; Yotsu-Yamashita, M, 2016
)
0.43

Dosage Studied

In a recent study, mice were dosed with saxitoxin and tetrodotoxin mixtures daily for 28 days showing toxicity at low concentrations. Analysis of the gut contents of mice dose with dcGTX1&4 showed the presence of decarbamoyl gonyautoxin 2&3, decarbAmoyl saxit toxin and decarbAMoyl neosaxitoxin. All of which are of greater toxicity.

ExcerptRelevanceReference
" On isolated frog sartorius muscle fibers, chiriquitoxin is equipotent with tetrodotoxin in blocking the Na+ channel, as shown by their identical dose-response relations on the maximum rate of rise of the action potential."( Tetrodotoxin, saxitoxin, chiriquitoxin: new perspectives on ionic channels.
Kao, CY, 1981
)
0.26
" Block was well described by single-site dose-response relationships with no indication of a subpopulation with "neuronal" affinity."( Cardiac sodium channels expressed in a peripheral neurotumor-derived cell line, RT4-B8.
Ambler, KS; Hanck, DA; Kyle, JW; Martin, RL; Zeng, D, 1996
)
0.29
" Dose-response curves for genistein indicated a half-maximum effect at 60 microM."( Direct block of voltage-sensitive sodium channels by genistein, a tyrosine kinase inhibitor.
Carlier, E; Couraud, F; Dargent, B; Guedin, D; Paillart, C, 1997
)
0.3
" Using the P53(def) transgenic mouse model male and female C57BL/6J hybrid mice were used to investigate potential cancer inducing effects from such oral dosing solutions."( Toxicological aspects of treatment to remove cyanobacterial toxins from drinking water determined using the heterozygous P53 transgenic mouse model.
Seawright, A; Senogles-Derham, PJ; Shahin, M; Shaw, G; Wickramisingh, W, 2003
)
0.32
" When the same dosage of tetrodotoxin (TTX) was similarly administered, all specimens died within 3-4h, suggesting that this species is not resistant to TTX."( Occurrence of paralytic shellfish toxins in Cambodian Mekong pufferfish Tetraodon turgidus: selective toxin accumulation in the skin.
Arakawa, O; Ngy, L; Tada, K; Takatani, T; Yu, CF, 2008
)
0.35
" These values are considerably below the concentration of saxitoxin that corresponds to the lethal dosage of 1 mg for an adult of average weight (70 kg)."( Detection and inactivation of saxitoxin in skim milk.
Deen, BD; Diez-Gonzalez, F; Fredrickson, NR; Labuza, TP; Lumor, SE; Ronningen, I; Smith, K, 2012
)
0.38
" Analysis of the gut contents of mice dosed with dcGTX1&4 showed the presence of decarbamoyl gonyautoxin 2&3, decarbamoyl saxitoxin and decarbamoyl neosaxitoxin, all of which are of greater toxicity."( Acute toxicity of decarbamoyl gonyautoxin 1&4 to mice by various routes of administration.
Boundy, MJ; Burger, E; Finch, S; Harwood, DT; Selwood, AI; Tommasi, E; van Ginkel, R; Waugh, C, 2021
)
0.62
"5 - 10 µg/L induced cytostasis and chromosome instability in a dose-response relationship."( In vitro and in silico assessment of cytotoxicity and chromosome instability induced by saxitoxin in human derived neural cell line.
Constante, JS; Conter, FU; Dihl, RR; Khateeb, JEA; Lehmann, M; Souza, AP; Yunes, JS, 2022
)
0.72
" In a recent study, mice were dosed with saxitoxin and tetrodotoxin mixtures daily for 28 days showing toxicity at low concentrations, which appeared to be at odds with other work."( A Sub-Acute Dosing Study of Saxitoxin and Tetrodotoxin Mixtures in Mice Suggests That the Current Paralytic Shellfish Toxin Regulatory Limit Is Fit for Purpose.
Boundy, MJ; Broadhurst, RB; Finch, SC; Harwood, DT; Munday, JS; Somchit, C; Sprosen, JM; Webb, NG, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
neurotoxinA poison that interferes with the functions of the nervous system.
toxinPoisonous substance produced by a biological organism such as a microbe, animal or plant.
sodium channel blockerAn agent that inhibits sodium influx through cell membranes.
marine metaboliteAny metabolite produced during a metabolic reaction in marine macro- and microorganisms.
cyanotoxinAny toxin produced by cyanobacteria (blue-green algae).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
alkaloidAny of the naturally occurring, basic nitrogen compounds (mostly heterocyclic) occurring mostly in the plant kingdom, but also found in bacteria, fungi, and animals. By extension, certain neutral compounds biogenetically related to basic alkaloids are also classed as alkaloids. Amino acids, peptides, proteins, nucleotides, nucleic acids, amino sugars and antibiotics are not normally regarded as alkaloids. Compounds in which the nitrogen is exocyclic (dopamine, mescaline, serotonin, etc.) are usually classed as amines rather than alkaloids.
pyrrolopurineAny organic heterotricyclic compound with a skeleton consisting of a pyrrole ring fused to a purine ring system.
ketone hydrateA 1,1-diol resulting from the formal addition of water to the carbonyl group of a ketone.
paralytic shellfish toxin
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium channel protein type 1 subunit alphaHomo sapiens (human)IC50 (µMol)0.00230.00232.82969.0000AID1525388
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC50 (µMol)0.01040.00013.507510.0000AID1525391; AID1875797
Sodium channel protein type 7 subunit alphaHomo sapiens (human)IC50 (µMol)0.41000.03603.73359.0000AID1525384
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)0.21000.00033.64849.2000AID1525392
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC50 (µMol)0.70200.00602.77499.0000AID1420157; AID1875809
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC50 (µMol)0.00100.00003.740110.0000AID1525389
Sodium channel protein type 3 subunit alphaHomo sapiens (human)IC50 (µMol)0.01300.00532.80859.0000AID1525390
Sodium channel protein type 11 subunit alphaHomo sapiens (human)IC50 (µMol)10.00000.03004.36959.0000AID1525446
Sodium channel protein type 8 subunit alphaHomo sapiens (human)IC50 (µMol)0.00110.00113.47059.0000AID1525393
Sodium channel protein type 10 subunit alphaHomo sapiens (human)IC50 (µMol)10.00000.00803.17529.0000AID1525394
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

Processvia Protein(s)Taxonomy
sodium ion transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
adult walking behaviorSodium channel protein type 1 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potential propagationSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuromuscular process controlling postureSodium channel protein type 1 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painSodium channel protein type 1 subunit alphaHomo sapiens (human)
establishment of localization in cellSodium channel protein type 1 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 1 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
regulation of presynaptic membrane potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 1 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
muscle contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
regulation of skeletal muscle contraction by action potentialSodium channel protein type 4 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
osmosensory signaling pathwaySodium channel protein type 7 subunit alphaHomo sapiens (human)
response to bacteriumSodium channel protein type 7 subunit alphaHomo sapiens (human)
cellular homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion homeostasisSodium channel protein type 7 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 7 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 7 subunit alphaHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
inflammatory responseSodium channel protein type 9 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 9 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 9 subunit alphaHomo sapiens (human)
post-embryonic developmentSodium channel protein type 9 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perceptionSodium channel protein type 9 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuron apoptotic processSodium channel protein type 2 subunit alphaHomo sapiens (human)
memorySodium channel protein type 2 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 2 subunit alphaHomo sapiens (human)
dentate gyrus developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 2 subunit alphaHomo sapiens (human)
cellular response to hypoxiaSodium channel protein type 2 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 3 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 3 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 3 subunit alphaHomo sapiens (human)
thigmotaxisSodium channel protein type 11 subunit alphaHomo sapiens (human)
acute inflammatory responseSodium channel protein type 11 subunit alphaHomo sapiens (human)
chronic inflammatory responseSodium channel protein type 11 subunit alphaHomo sapiens (human)
axonogenesisSodium channel protein type 11 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to heatSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to xenobiotic stimulusSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to high light intensitySodium channel protein type 11 subunit alphaHomo sapiens (human)
protein kinase A signalingSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to auditory stimulusSodium channel protein type 11 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 11 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to prostaglandin ESodium channel protein type 11 subunit alphaHomo sapiens (human)
thermosensory behaviorSodium channel protein type 11 subunit alphaHomo sapiens (human)
mast cell degranulationSodium channel protein type 11 subunit alphaHomo sapiens (human)
cell motilitySodium channel protein type 11 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painSodium channel protein type 11 subunit alphaHomo sapiens (human)
reflexSodium channel protein type 11 subunit alphaHomo sapiens (human)
micturitionSodium channel protein type 11 subunit alphaHomo sapiens (human)
skeletal muscle organ developmentSodium channel protein type 11 subunit alphaHomo sapiens (human)
artery developmentSodium channel protein type 11 subunit alphaHomo sapiens (human)
behavioral response to acetic acid induced painSodium channel protein type 11 subunit alphaHomo sapiens (human)
behavioral response to formalin induced painSodium channel protein type 11 subunit alphaHomo sapiens (human)
cellular response to coldSodium channel protein type 11 subunit alphaHomo sapiens (human)
calcium ion transmembrane transportSodium channel protein type 11 subunit alphaHomo sapiens (human)
response to nitric oxideSodium channel protein type 11 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 11 subunit alphaHomo sapiens (human)
action potential initiationSodium channel protein type 11 subunit alphaHomo sapiens (human)
sensory perception of itchSodium channel protein type 11 subunit alphaHomo sapiens (human)
calcitonin gene-related peptide receptor signaling pathwaySodium channel protein type 11 subunit alphaHomo sapiens (human)
small intestine smooth muscle contractionSodium channel protein type 11 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 11 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 11 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
peripheral nervous system developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 8 subunit alphaHomo sapiens (human)
optic nerve developmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 8 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 8 subunit alphaHomo sapiens (human)
regulation of heart rateSodium channel protein type 10 subunit alphaHomo sapiens (human)
sensory perceptionSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of monoatomic ion transmembrane transportSodium channel protein type 10 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 10 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of cardiac muscle contractionSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 10 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
regulation of presynaptic membrane potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
voltage-gated sodium channel activitySodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialSodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 4 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 4 subunit alphaHomo sapiens (human)
sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 7 subunit alphaHomo sapiens (human)
osmolarity-sensing monoatomic cation channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 9 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 2 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 11 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 8 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
ATP bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
sodium ion bindingSodium channel protein type 8 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 10 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 10 subunit alphaHomo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 1 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 1 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 1 subunit alphaHomo sapiens (human)
nuclear bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 1 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 1 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 1 subunit alphaHomo sapiens (human)
neuronal cell bodySodium channel protein type 1 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 1 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 1 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 4 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 4 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 7 subunit alphaHomo sapiens (human)
glial cell projectionSodium channel protein type 7 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 7 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 9 subunit alphaHomo sapiens (human)
axonSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 9 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 2 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 2 subunit alphaHomo sapiens (human)
axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 2 subunit alphaHomo sapiens (human)
paranode region of axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 2 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
sarcoplasmSodium channel protein type 3 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 3 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 11 subunit alphaHomo sapiens (human)
axonSodium channel protein type 11 subunit alphaHomo sapiens (human)
neuronal cell bodySodium channel protein type 11 subunit alphaHomo sapiens (human)
axonal growth coneSodium channel protein type 11 subunit alphaHomo sapiens (human)
C-fiberSodium channel protein type 11 subunit alphaHomo sapiens (human)
extracellular exosomeSodium channel protein type 11 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 11 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 8 subunit alphaHomo sapiens (human)
cell junctionSodium channel protein type 8 subunit alphaHomo sapiens (human)
axonSodium channel protein type 8 subunit alphaHomo sapiens (human)
cytoplasmic vesicleSodium channel protein type 8 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 8 subunit alphaHomo sapiens (human)
axon initial segmentSodium channel protein type 8 subunit alphaHomo sapiens (human)
presynaptic active zone membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
parallel fiber to Purkinje cell synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
postsynaptic density membraneSodium channel protein type 8 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 8 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 8 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 10 subunit alphaHomo sapiens (human)
axonSodium channel protein type 10 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 10 subunit alphaHomo sapiens (human)
extracellular exosomeSodium channel protein type 10 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 10 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 10 subunit alphaHomo sapiens (human)
clathrin complexSodium channel protein type 10 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID1525401Selectivity index, ratio of IC50 for inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1875809Inhibition of human Nav1.7 expressed in CHO cells at -100 mV holding potential by electrophysiology whole cell patch clamp technique2022ACS medicinal chemistry letters, Nov-10, Volume: 13, Issue:11
Discovery of Selective Inhibitors of Na
AID1525390Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525397Selectivity index, ratio of IC50 for inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID362643Toxicity in mouse at 2483 MU/umol, ip2008Journal of natural products, Sep, Volume: 71, Issue:9
Isolation and structure elucidation of new and unusual saxitoxin analogues from mussels.
AID1525388Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1420157Inhibition of human Nav1.7 expressed in CHO cells at holding potential of -100 mV by patch-clamp electrophysiology method2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Na
AID1525395Selectivity index, ratio of IC50 for inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525393Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525389Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1875810Inhibition of human Nav1.7 T1398M-I1399D mutant expressed in CHO cells at -100 mV holding potential by electrophysiology whole cell patch clamp technique2022ACS medicinal chemistry letters, Nov-10, Volume: 13, Issue:11
Discovery of Selective Inhibitors of Na
AID1525396Selectivity index, ratio of IC50 for inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525398Selectivity index, ratio of IC50 for inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525384Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525400Selectivity index, ratio of IC50 for inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525391Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525392Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525446Inhibition of human Nav1.9 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525394Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1525399Selectivity index, ratio of IC50 for inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1875797Inhibition of human Nav1.4 expressed in HEK293 cells by whole cell patch clamp electrophysiology recording2022ACS medicinal chemistry letters, Nov-10, Volume: 13, Issue:11
Discovery of Selective Inhibitors of Na
AID1525447Selectivity index, ratio of IC50 for inhibition of human Nav1.9 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na
AID1346781Rat Nav1.4 (Voltage-gated sodium channels)2001Biophysical journal, Feb, Volume: 80, Issue:2
Specific neosaxitoxin interactions with the Na+ channel outer vestibule determined by mutant cycle analysis.
AID1346731Rat Nav1.2 (Voltage-gated sodium channels)2005Nature, Apr-07, Volume: 434, Issue:7034
Sodium channel mutation leading to saxitoxin resistance in clams increases risk of PSP.
AID1346772Rat Nav1.5 (Voltage-gated sodium channels)1990FEBS letters, Nov-26, Volume: 275, Issue:1-2
Functional expression of the rat heart I Na+ channel isoform. Demonstration of properties characteristic of native cardiac Na+ channels.
AID1346749Human Nav1.7 (Voltage-gated sodium channels)2012Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 109, Issue:44
Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7) [corrected].
AID1346772Rat Nav1.5 (Voltage-gated sodium channels)1996The American journal of physiology, May, Volume: 270, Issue:5 Pt 1
Cardiac sodium channels expressed in a peripheral neurotumor-derived cell line, RT4-B8.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,283)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990308 (24.01)18.7374
1990's245 (19.10)18.2507
2000's254 (19.80)29.6817
2010's334 (26.03)24.3611
2020's142 (11.07)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (0.74%)5.53%
Reviews103 (7.60%)6.00%
Case Studies23 (1.70%)4.05%
Observational0 (0.00%)0.25%
Other1,219 (89.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]