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ASIC2

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 685

Nomenclature: ASIC2

Family: Acid-sensing (proton-gated) ion channels (ASICs)

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 512 17q11.2-q12 ASIC2 acid sensing ion channel subunit 2
Mouse 2 512 11 48.43 cM Asic2 acid-sensing (proton-gated) ion channel 2
Rat 2 512 10q26 Asic2 acid sensing ion channel subunit 2
Previous and Unofficial Names Click here for help
ACCN | ACCN1 | acid-sensing ion channel 2 | acid-sensing (proton-gated) ion channel 2 | acid sensing (proton gated) ion channel 2 | amiloride-sensitive brain sodium channel 2 | amiloride-sensitive cation channel 1 | amiloride-sensitive cation channel 1, neuronal | ASIC2a | BNaC1 | BNaC1a | BNC1 | BNC1k | brain sodium channel 1 | degenerin | MDEG
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Functional Characteristics Click here for help
γ=10.4-13.4 pS
PNa/PK =10, PNa/PCa = 20
rapid activation rate, moderate inactivation rate (3.3-5.5 s) @ pH 5
Natural/Endogenous Ligands Click here for help
H+

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Activators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
Extracellular H+ Click here for species-specific activity table Ligand is endogenous in the given species Hs - ~4.1 – 5.0 pEC50 - no
pEC50 ~4.1 – 5.0 (EC50 ~8x10-5 – 1x10-5 M)
Not voltage dependent
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
diminazene Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs - no ~6.1 pIC50 - no 4
pIC50 ~6.1 [4]
Not voltage dependent
amiloride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs - no 4.6 pIC50 - no 9
pIC50 4.6 (IC50 2.8x10-5 M) [9]
Not voltage dependent
A-317567 Small molecule or natural product Click here for species-specific activity table Hs - no ~4.5 pIC50 - no 3
pIC50 ~4.5 (IC50 ~3x10-5 M) [3]
Not voltage dependent
nafamostat Small molecule or natural product Approved drug Click here for species-specific activity table Hs - no ~4.2 pIC50 - no 8
pIC50 ~4.2 (IC50 ~7x10-5 M) [8]
Not voltage dependent
Cd2+ Click here for species-specific activity table Hs - no ~3.0 pIC50 - no 7
pIC50 ~3.0 (IC50 ~1x10-3 M) Partial inhibition [7]
Not voltage dependent
Immunopharmacology Comments
Non-steroidal anti-inflammatory drugs (NSAIDs) are direct inhibitors of ASIC currents (reviewed in [1]). Inflammatory conditions and particular pro-inflammatory mediators such as arachidonic acid induce overexpression of ASIC-encoding genes and enhance ASIC currents [2,5-6]. The sustained current component mediated by ASIC3 is potentiated by hypertonic solutions in a manner that is synergistic with the effect of arachidonic acid [2].

References

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1. Baron A, Lingueglia E. (2015) Pharmacology of acid-sensing ion channels - Physiological and therapeutical perspectives. Neuropharmacology, 94: 19-35. [PMID:25613302]

2. Deval E, Noël J, Lay N, Alloui A, Diochot S, Friend V, Jodar M, Lazdunski M, Lingueglia E. (2008) ASIC3, a sensor of acidic and primary inflammatory pain. EMBO J., 27 (22): 3047-55. [PMID:18923424]

3. Dubé GR, Lehto SG, Breese NM, Baker SJ, Wang X, Matulenko MA, Honoré P, Stewart AO, Moreland RB, Brioni JD. (2005) Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain, 117 (1-2): 88-96. [PMID:16061325]

4. Lee JYP, Saez NJ, Cristofori-Armstrong B, Anangi R, King GF, Smith MT, Rash LD. (2018) Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain. Br. J. Pharmacol., 175 (12): 2204-2218. [PMID:29134638]

5. Mamet J, Baron A, Lazdunski M, Voilley N. (2002) Proinflammatory mediators, stimulators of sensory neuron excitability via the expression of acid-sensing ion channels. J. Neurosci., 22 (24): 10662-70. [PMID:12486159]

6. Smith ES, Cadiou H, McNaughton PA. (2007) Arachidonic acid potentiates acid-sensing ion channels in rat sensory neurons by a direct action. Neuroscience, 145 (2): 686-98. [PMID:17258862]

7. Staruschenko A, Dorofeeva NA, Bolshakov KV, Stockand JD. (2007) Subunit-dependent cadmium and nickel inhibition of acid-sensing ion channels. Dev Neurobiol, 67 (1): 97-107. [PMID:17443775]

8. Ugawa S, Ishida Y, Ueda T, Inoue K, Nagao M, Shimada S. (2007) Nafamostat mesilate reversibly blocks acid-sensing ion channel currents. Biochem Biophys Res Commun, 363 (1): 203-8. [PMID:17826743]

9. Waldmann R, Champigny G, Voilley N, Lauritzen I, Lazdunski M. (1996) The mammalian degenerin MDEG, an amiloride-sensitive cation channel activated by mutations causing neurodegeneration in Caenorhabditis elegans. J. Biol. Chem., 271 (18): 10433-6. [PMID:8631835]

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