ASIC2 | Acid-sensing (proton-gated) ion channels (ASICs) | IUPHAR/BPS Guide to PHARMACOLOGY

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ASIC2

target has curated data in GtoImmuPdb

Target id: 685

Nomenclature: ASIC2

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

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - 17q11.2-q12 ASIC2 acid sensing ion channel subunit 2
Mouse - - 11 B5 Asic2 acid-sensing (proton-gated) ion channel 2
Rat - - 10q26 Asic2 acid sensing ion channel subunit 2
Previous and Unofficial Names
BNaC1 | BNC1 | ACCN | ACCN1 | ASIC2a | amiloride-sensitive cation channel 1, neuronal | degenerin | acid-sensing ion channel 2 | amiloride-sensitive brain sodium channel 2 | amiloride-sensitive cation channel 1 | BNC1k | brain sodium channel 1 | BNaC1a | acid-sensing (proton-gated) ion channel 2 | acid sensing (proton gated) ion channel 2
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Functional Characteristics
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
H+

Download all structure-activity data for this target as a CSV file

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+ 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 Hs - no ~6.1 pIC50 - no 3
pIC50 ~6.1 [3]
Not voltage dependent
amiloride Hs - no 4.6 pIC50 - no
pIC50 4.6 (IC50 2.8x10-5 M)
Not voltage dependent
A-317567 Hs - no ~4.5 pIC50 - no
pIC50 ~4.5 (IC50 ~3x10-5 M)
Not voltage dependent
nafamostat Hs - no ~4.2 pIC50 - no
pIC50 ~4.2 (IC50 ~7x10-5 M)
Not voltage dependent
Cd2+ Hs - no ~3.0 pIC50 - no
pIC50 ~3.0 (IC50 ~1x10-3 M)
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 [2,4-5]. 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. 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]

4. 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]

5. 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]

Contributors

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