ASIC3 | Acid-sensing (proton-gated) ion channels (ASICs) | IUPHAR/BPS Guide to PHARMACOLOGY

ASIC3

Target id: 686

Nomenclature: ASIC3

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 ASIC3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - 7q35 ASIC3 acid sensing ion channel subunit 3
Mouse - - 5 A3 Asic3 acid-sensing (proton-gated) ion channel 3
Rat - - 4q11 Asic3 acid sensing ion channel subunit 3
Previous and Unofficial Names
DRASIC | TNaC1 | ACCN3 | amiloride-sensitive cation channel 3, testis | testis sodium channel 1 | acid sensing ion channel 3 | dorsal root ASIC | acid-sensing (proton-gated) ion channel 3 | acid sensing (proton gated) ion channel 3
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Functional Characteristics
γ~ 13-15 pS;
biphasic response consisting of rapidly inactivating transient and sustained components;
very rapid activation (<5 ms) and inactivation (0.4 s);
fast recovery (0.4-0.6 s) @ pH 7.4, transient component partially inactivated at pH 7.2
Natural/Endogenous Ligands
H+

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

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Concentration range (M) Voltage-dependent (mV) Reference
Extracellular H+ Hs - ~3.5 – 6.7 pEC50 - no
pEC50 ~6.2 – 6.7 (EC50 ~6.3x10-7 – 2x10-7 M) transient component
Not voltage dependent
pEC50 ~3.5 – 4.3 (EC50 ~3.5x10-4 – 5x10-5 M) sustained component
Not voltage dependent
GMQ Hs - ~3.0 pEC50 - no
pEC50 ~3.0 (EC50 ~1x10-3 M) largly non-desensitizing; at pH 7.4
Not voltage dependent
arcaine Hs - ~2.9 pEC50 - no
pEC50 ~2.9 (EC50 ~1.2x10-3 M) at pH 7.4
Not voltage dependent
agmatine Hs - ~2.0 pEC50 - no
pEC50 ~2.0 (EC50 ~9.8x10-3 M) at pH 7.4
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
APETx2 Hs - no 7.2 pIC50 - no
pIC50 7.2 (IC50 6.3x10-8 M) transient component only
Not voltage dependent
nafamostat Hs - no ~5.6 pIC50 - no
pIC50 ~5.6 (IC50 ~2.5x10-6 M) transient component
Not voltage dependent
A-317567 Hs - no ~5.0 pIC50 - no
pIC50 ~5.0 (IC50 ~1x10-5 M)
Not voltage dependent
amiloride Hs - no 4.2 – 4.8 pIC50 - no
pIC50 4.2 – 4.8 (IC50 6.3x10-5 – 1.6x10-5 M) transient component only - sustained component enhanced by 200μM amiloride at pH 4
Not voltage dependent
Gd3+ Hs - no 4.4 pIC50 - no
pIC50 4.4 (IC50 4x10-5 M)
Not voltage dependent
Zn2+ Hs - no 4.2 pIC50 - no
pIC50 4.2 (IC50 6.1x10-5 M)
Not voltage dependent
diclofenac Hs - no 4.0 pIC50 - no
pIC50 4.0 (IC50 9.2x10-5 M) sustained component
Not voltage dependent
aspirin Hs - no 4.0 pIC50 - no 1
pIC50 4.0 (IC50 9.2x10-5 M) sustained component [1]
Not voltage dependent
salicylic acid Hs - no 3.6 pIC50 - no
pIC50 3.6 (IC50 2.6x10-4 M) sustained component
Not voltage dependent

References

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1. 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): ASIC3. Last modified on 13/03/2018. Accessed on 19/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=686.