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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, 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]

  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.