Skip to main content

Table 1 Basic channel properties, activators and inhibitors of ASICs

From: Acid-sensing ion channels: trafficking and synaptic function

Gene Protein pH50 Agonist (EC50) Antagonist (IC50) Ions passed References
ASIC1
(ACCN2)
ASIC1a 6.2–6.8 MitTx (9.4 nM) PcTx1 (~1 nM) Na+ > Ca2+ [5, 12, 13, 2227]
     Mambalgin (55 nM)   
     Sevanol (2.2 mM)   
     A-317567 (2 μM)   
  ASIC1b ~6.0 (mouse) MitTx (23 nM) Mambalgin (192 nM) mouse: Na+ human: Na+ > Ca2+ [6, 7, 12, 13, 22, 24, 28]
   ~6.2 (human)     
ASIC2 (ACCN1) ASIC2a 4.5–4.9 Minimal activa-tion by MitTx A-317567 (29 μM) Na+ [12, 15, 22, 25, 2931]
  ASIC2b N/A    -- [2931]
ASIC3 ASIC3 ~6.6 GMQ (0.35 mM) APETx2 (63 nM) Na+ [13, 22, 25, 3236]
    MitTx (830 nM) Sevanol (0.35 mM)   
     A-317567 (9.5 μM)   
ASIC4 ASIC4 N/A    -- [37]
Heteromeric channels 1a + 1b 6.0   Mambalgin (72 nM) Na+ [15]
  1a + 2a 5.5–6.1   Mambalgin (246 nM) Na+ [12, 15, 24, 26]
  1a + 2b Same as ASIC1a   Mambalgin (61 nM) PcTx1 (~3 nM) Na+ > Ca2+ [9, 15, 24]
  1a + 3 6.3–6,6    Na+ [12, 15]
  1b + 3 6.0    Na+ [15]
  1b + 2a 4.9    Na+ [15]
  2a + 3 5.7–6.1    Na+ [12, 15]
  2b + 3 6.5   APETx2 (117 nM) Na+ [15, 33, 36]
  1. Note: amiloride is not included in the table because it functions as a universal blocker for ASICs and many other ion channels, such as ENaCs and sodium/hydrogen exchangers.