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.