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. 2013 Jan 2;6:1. doi: 10.1186/1756-6606-6-1

Table 1.

Basic channel properties, activators and inhibitors of ASICs

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+
[5,12,13,22-27]
 
 
 
 
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+
[12,15,22,25,29-31]
 
ASIC2b
N/A
 
 
--
[29-31]
ASIC3
ASIC3
~6.6
GMQ (0.35 mM)
APETx2 (63 nM)
Na+
[13,22,25,32-36]
 
 
 
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]

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.