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. 2013 Dec 17;170(8):1607–1651. doi: 10.1111/bph.12447
Nomenclature CatSper1 CatSper2 CatSper3 CatSper4
HGNC, UniProt CATSPER1, Q8NEC5 CATSPER2, Q96P56 CATSPER3, Q86XQ3 CATSPER4, Q7RTX7
Activators CatSper1 is constitutively active, weakly facilitated by membrane depolarisation, strongly augmented by intracellular alkalinisation. In human, but not mouse, spermatozoa progesterone (EC50 ∼ 8 nM) also potentiates the CatSper current (ICatSper).
Channel Blockers (IC50) NNC55-0396 (2x10-6 – 1x10-5 M), ruthenium red (1x10-5 M), HC056456 (2x10-5 M), mibefradil (3x10-5 M), Cd2+ (2x10-4 M), Ni2+ (3x10-4 M)
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 [V½ @ pH 6.0 = +87 mV (mouse); V½ @ pH 7.5 = +11mV (mouse) or pH 7.4 = +85 mV (human)] Required for ICatSper Required for ICatSper Required for ICatSper