ASIC1 | Acid-sensing (proton-gated) ion channels (ASICs) | IUPHAR/BPS Guide to PHARMACOLOGY

ASIC1

Target id: 684

Nomenclature: ASIC1

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

   GtoImmuPdb view: OFF :     Currently no data for ASIC1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - 12q12 ASIC1 acid sensing ion channel subunit 1
Mouse - - 15 F3 Asic1 acid-sensing (proton-gated) ion channel 1
Rat - - 7q36 Asic1 acid sensing ion channel subunit 1
Previous and Unofficial Names
BNaC2 | ACCN2 | amiloride-sensitive cation channel 2, neuronal | acid-sensing ion channel 1 | brain sodium channel 2 | ASIC1 beta | ASICalpha | acid-sensing (proton-gated) ion channel 1 | acid sensing (proton gated) ion channel 1
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of chicken (Gallus gallus) ASIC1a with Texas coral snake toxin (MitTx).
PDB Id:  4NTW
Resolution:  2.07Å
Species:  Chicken
References:  1
Functional Characteristics
ASIC1a: γ ~14pS
PNa/PK = 5-13, PNa/PCa =2.5
rapid activation rate (5.8-13.7 ms), rapid inactivation rate (1.2-4 s) @ pH 6.0, slow recovery (5.3-13s) @ pH 7.4
ASIC1b: γ ~ 19 pS
PNa/PK =14.0, PNa >> PCa
rapid activation rate (9.9 ms), rapid inactivation rate (0.9-1.7 s) @ pH 6.0, slow recovery (4.4-7.7 s) @ pH 7.4
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 Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
Extracellular H+ Hs - ~5.1 – 6.8 pEC50 - no
pEC50 ~6.2 – 6.8 (EC50 ~6.3x10-7 – 1.6x10-7 M) ASIC1a
Not voltage dependent
pEC50 ~5.1 – 6.2 (EC50 ~8x10-6 – 6.3x10-7 M) ASIC1b
Not voltage dependent
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
psalmotoxin 1 Hs - no 9.0 pIC50 - no
pIC50 9.0 (IC50 9x10-10 M) ASIC1a
Not voltage dependent
Zn2+ Hs - no ~8.2 pIC50 - no
pIC50 ~8.2 (IC50 ~7x10-9 M) ASIC1a
Not voltage dependent
A-317567 Rn - no ~5.7 pIC50 - no 2
pIC50 ~5.7 (IC50 ~2x10-6 M) ASIC1a [2]
Not voltage dependent
Pb2+ Hs - no ~5.4 – 5.8 pIC50 - no
pIC50 ~5.8 (IC50 ~1.5x10-6 M) ASIC1b
Not voltage dependent
pIC50 ~5.4 (IC50 ~4x10-6 M) ASIC1a
Not voltage dependent
benzamil Hs - no 5.0 pIC50 - no
pIC50 5.0 (IC50 1x10-5 M) ASIC1a
Not voltage dependent
ethylisopropylamiloride Hs - no 5.0 pIC50 - no
pIC50 5.0 (IC50 1x10-5 M) ASIC1a
Not voltage dependent
nafamostat Hs - no ~4.9 pIC50 - no
pIC50 ~4.9 (IC50 ~1.3x10-5 M) ASIC1a
Not voltage dependent
amiloride Hs - no 4.6 – 5.0 pIC50 - no
pIC50 5.0 (IC50 1x10-5 M) ASIC1a
Not voltage dependent
pIC50 4.6 – 4.7 (IC50 2.3x10-5 – 2.1x10-5 M) ASIC1b
Not voltage dependent
ibuprofen Hs - no ~3.5 pIC50 - no
pIC50 ~3.5 (IC50 ~3.5x10-4 M) ASIC1a
Not voltage dependent
flurbiprofen Rn - no 3.5 pIC50 - no 3
pIC50 3.5 (IC50 3.5x10-4 M) ASIC1a [3]
Not voltage dependent
Ni2+ Hs - no ~3.2 pIC50 - no
pIC50 ~3.2 (IC50 ~6x10-4 M) ASIC1a
Not voltage dependent
View species-specific channel blocker tables
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]psalmotoxin 1 Hs - 9.7 pKd
pKd 9.7 (Kd 2.13x10-10 M) ASIC1a

References

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1. Baconguis I, Bohlen CJ, Goehring A, Julius D, Gouaux E. (2014) X-ray structure of acid-sensing ion channel 1-snake toxin complex reveals open state of a Na(+)-selective channel. Cell, 156 (4): 717-29. [PMID:24507937]

2. 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]

3. Voilley N, de Weille J, Mamet J, Lazdunski M. (2001) Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors. J. Neurosci., 21 (20): 8026-33. [PMID:11588175]

Contributors

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How to cite this page

Stephan Kellenberger, Laurent Schild.
Acid-sensing (proton-gated) ion channels (ASICs): ASIC1. Last modified on 13/03/2018. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=684.