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. 2019 Nov 11;176(Suppl 1):S142–S228. doi: 10.1111/bph.14749
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=686
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:101, http://www.uniprot.org/uniprot/Q9UHC3
Endogenous activators Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 + (transient component) (pEC50 ∼6.2–6.7), Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 + (sustained component) (pEC50 ∼3.5–4.3)
Activators http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4203 (largly non‐desensitizing; at pH 7.4) (pEC50 ∼3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4137 (at pH 7.4) (pEC50 ∼2.9), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4127 (at pH 7.4) (pEC50 ∼2)
Channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4135 (transient component only) (pIC50 7.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10307 (pIC50 ∼6.5) [http://www.ncbi.nlm.nih.gov/pubmed/29134638?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4116 (pIC50 6) [http://www.ncbi.nlm.nih.gov/pubmed/22778804?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4262 (transient component) (pIC50 ∼5.6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2421 (transient component only ‐ sustained component enhanced by 200μM amiloride at pH 4) (pIC50 4.2–4.8), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2426 (pIC50 4.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (pIC50 4.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4139 (sustained component) (pIC50 4) [http://www.ncbi.nlm.nih.gov/pubmed/11588175?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2714 (sustained component) (pIC50 4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4306 (sustained component) (pIC50 3.6)
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
Comments ASIC3 is activated by Mit‐Toxin (pEC50 6.1) [http://www.ncbi.nlm.nih.gov/pubmed/22094702?dopt=AbstractPlus].