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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=394 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=395 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=396 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=399
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2148, http://www.uniprot.org/uniprot/P29973 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2149, http://www.uniprot.org/uniprot/Q16280 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2150, http://www.uniprot.org/uniprot/Q16281 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2153, http://www.uniprot.org/uniprot/Q9NQW8
Activators http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2347 (EC50 30 μM) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2352 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2347 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2352 (EC50 1 μM) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2347 (EC50 30 μM) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2352 –
Inhibitors – – http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2349 (high affinity binding requires presence of CNGB subunits) –
Channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2313 (Antagonist) (pIC50 6.7) [0mV] [http://www.ncbi.nlm.nih.gov/pubmed/12508052?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2349 (Antagonist) (pK i 4) [−80mV – 80mV] [http://www.ncbi.nlm.nih.gov/pubmed/7682292?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2313 (Antagonist) (pIC50 5.6) [0mV] [http://www.ncbi.nlm.nih.gov/pubmed/14981138?dopt=AbstractPlus] – http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2349 (Antagonist) (pIC50 5.5) [0mV] [http://www.ncbi.nlm.nih.gov/pubmed/10662822?dopt=AbstractPlus] – Mouse
Functional Characteristics γ = 25‐30 pS PCa/PNa = 3.1 γ = 35 pS PCa/PNa = 6.8 γ = 40 pS P Ca/P Na = 10.9 –