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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=684 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=685
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:100, http://www.uniprot.org/uniprot/P78348 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:99, http://www.uniprot.org/uniprot/Q16515
Endogenous activators Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 + (ASIC1a) (pEC50 ∼6.2–6.8), Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 + (ASIC1b) (pEC50 ∼5.1–6.2) Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 + (pEC50 ∼4.1–5)
Channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10306 (ASIC1a) (pIC50 ∼9.3) [http://www.ncbi.nlm.nih.gov/pubmed/28320947?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4292 (ASIC1a) (pIC50 9), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10305 (ASIC1a) (pIC50 ∼8.5) [http://www.ncbi.nlm.nih.gov/pubmed/28327374?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (ASIC1a) (pIC50 ∼8.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10308 (ASIC1a) (pIC50 ∼7.3) [http://www.ncbi.nlm.nih.gov/pubmed/23034652?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10308 (ASIC1b) (pIC50 ∼7) [http://www.ncbi.nlm.nih.gov/pubmed/23624383?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10307 (ASIC1a & ASIC1b) (pIC50 ∼6.5) [http://www.ncbi.nlm.nih.gov/pubmed/29134638?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2525 (ASIC1b) (pIC50 ∼5.8), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4116 (ASIC1a) (pIC50 ∼5.7) [http://www.ncbi.nlm.nih.gov/pubmed/16061325?dopt=AbstractPlus] – Rat, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2525 (ASIC1a) (pIC50 ∼5.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2421 (ASIC1a) (pIC50 5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4145 (ASIC1a) (pIC50 5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4186 (ASIC1a) (pIC50 5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4262 (ASIC1a) (pIC50 ∼4.9), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2421 (ASIC1b) (pIC50 4.6–4.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4194 (ASIC1a) (pIC50 3.5) [http://www.ncbi.nlm.nih.gov/pubmed/11588175?dopt=AbstractPlus] – Rat, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2713 (ASIC1a) (pIC50 ∼3.5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2476 (ASIC1a) (pIC50 ∼3.2) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10307 (pIC50 ∼6.1) [http://www.ncbi.nlm.nih.gov/pubmed/29134638?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2421 (pIC50 4.6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4116 (pIC50 ∼4.5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4262 (pIC50 ∼4.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2440 (pIC50 ∼3)
Labelled ligands http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4073 (ASIC1a) (pK d 9.7)
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 = γ10.4‐13.4 pS PNa/PK =10, PNa/PCa = 20 rapid activation rate, moderate inactivation rate (3.3‐5.5 s) @ pH 5
Comments ASIC1a and ASIC1b are activated by the heteromeric Texas coral snake toxin MitTx, with pEC50 values of 8 and 7.6 respectively [http://www.ncbi.nlm.nih.gov/pubmed/22094702?dopt=AbstractPlus]. ASIC2 is also blocked by diarylamidines