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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=388 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=389 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=390 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=391
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:17116, http://www.uniprot.org/uniprot/Q8NEC5 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:18810, http://www.uniprot.org/uniprot/Q96P56 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:20819, http://www.uniprot.org/uniprot/Q86XQ3 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:23220, http://www.uniprot.org/uniprot/Q7RTX7
Activators CatSper1 is constitutively active, weakly facilitated by membrane depolarisation, strongly augmented by intracellular alkalinisation. In human, but not mouse, progesterone (EC50 8 nM) also potentiates the CatSper current (ICatSper). [http://www.ncbi.nlm.nih.gov/pubmed/21412339?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/21412338?dopt=AbstractPlus]
Channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2432 (Inhibition) (pIC50 5) [http://www.ncbi.nlm.nih.gov/pubmed/16467839?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4212 (pIC50 4.7) [http://www.ncbi.nlm.nih.gov/pubmed/19718436?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2440 (Inhibition) (pIC50 3.7) [http://www.ncbi.nlm.nih.gov/pubmed/16467839?dopt=AbstractPlus] – Mouse, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2476 (Inhibition) (pIC50 3.5) [http://www.ncbi.nlm.nih.gov/pubmed/16467839?dopt=AbstractPlus] – Mouse
Selective channel blockers http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4269 (Inhibition) (pIC50 5.7) [−80mV – 80mV] [http://www.ncbi.nlm.nih.gov/pubmed/21412339?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/21412338?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2522 (Inhibition) (pIC50 4.4–4.5) [http://www.ncbi.nlm.nih.gov/pubmed/21412338?dopt=AbstractPlus]
Functional Characteristics Calcium selective ion channel (Ba2+>Ca2+Mg2+Na+); quasilinear monovalent cation current in the absence of extracellular divalent cations; alkalinization shifts the voltage‐dependence of activation towards negative potentials [V @ pH 6.0 = +87 mV (mouse); V @ pH 7.5 = +11mV (mouse) or pH 7.4 = +85 mV (human)]; required for ICatSper and male fertility (mouse and human) Required for ICatSper and male fertility (mouse and human) Required for ICatSper and male fertility (mouse) Required for ICatSper and male fertility (mouse)