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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=423 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=424 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=425 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=426
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4326, http://www.uniprot.org/uniprot/P23415 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4327, http://www.uniprot.org/uniprot/P23416 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:4328, http://www.uniprot.org/uniprot/O75311 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:31715, http://www.uniprot.org/uniprot/Q5JXX5
Selective agonists (potency order) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=727 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2365 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2379 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=727 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2365 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2379 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=727 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2365 > http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2379 –
Selective antagonists http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4201 (pIC50 6.1), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4290 (pK i 5.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2514 (pIC50 5.5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2366 (pIC50 4.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=260 (pK i 4.1), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2367 (pIC50 3.5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=746 (weak inhibition), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4289, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=347 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=731 (pIC50 7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=733 (pIC50 6.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=746 (pIC50 6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4201 (pIC50 5.6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4290 (pK i 5.3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2366 (pIC50 5.1), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=260 (pK i 4.9), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2367 (pIC50 4.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2361 (pIC50 3.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4289, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=347 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=731 (pIC50 7.3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=746 (pIC50 7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=733 (pIC50 7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4072 (pIC50 5.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2514 (pIC50 4.5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=347 –
Channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1862 (pIC50 5.1–6.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2368 (pIC50 5.9) [http://www.ncbi.nlm.nih.gov/pubmed/8090751?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4286 (pIC50 5.3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2291 (pIC50 5.3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4051 (pIC50 5.2) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2291 (pIC50 6.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4051 (pIC50 5.6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1862 (pIC50 4.9–5.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4286 (pIC50 4.9), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2368 (pIC50 >4.7) [http://www.ncbi.nlm.nih.gov/pubmed/8090751?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2291 (pIC50 6.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1862 (pIC50 5.7), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4286 (pIC50 5.2), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4051 (block is weaker when β subunit is co‐expressed) –
Endogenous allosteric modulators http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (Potentiation) (pEC50 7.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4164 (Inhibition) (pIC50 4.8–5.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (Inhibition) (pIC50 4.8), Extracellular http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2346 (Inhibition) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (Potentiation) (pEC50 6.3), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4164 (Inhibition) (pIC50 4.8), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (Inhibition) (pIC50 3.4) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4164 (Inhibition) (pIC50 5), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=566 (Inhibition) (pIC50 3.8) –
Selective allosteric modulators http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2364 (Potentiation) (pEC50 7.4), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=731 (Potentiation) (pEC50 6.6), http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2424 (Potentiation) (pEC50 ∼5.5) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2424 (Potentiation) (pEC50 ∼6) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2424 (Potentiation) (pEC50 ∼5.3) –
Labelled ligands http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2360 (Antagonist) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2360 (Antagonist) http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2360 (Antagonist) –
Functional Characteristics γ = 86 pS (main state); (+ β = 44 pS) γ = 111 pS (main state); (+ β = 54 pS) γ = 105 pS (main state); (+ β = 48) –