5-HT3A
|
|
|
Hs |
Allosteric modulator |
Negative |
- |
- |
1x10-4 - 1x10-2 |
3,27 |
|
⤷ |
Conc range: 1x10-4 - 1x10-2 M
Decreased single channel conductance, increased channel activation rate, increased deactivation rate, increased desensitization rate, decrease in agonist apparent affinity.
[3,27]
|
5-HT3A
|
|
|
Mm |
Allosteric modulator |
Negative |
- |
- |
1x10-4 - 1x10-2 |
9,16,29 |
|
⤷ |
Conc range: 1x10-4 - 1x10-2 M
Decreased single channel conductance, increased channel activation rate, increased deactivation rate, increased desensitization rate, decrease in agonist apparent affinity.
[9,16,29]
|
TRPP2
|
|
|
Hs |
Activator (Intracellular Ca2+) |
Agonist |
- |
- |
5x10-3 |
5 |
|
⤷ |
Conc range: 5x10-3 M
[5]
Voltage:
-150.0 – 100.0 mV
Conc range: 5x10-3 M
[5]
Voltage:
-60.0 – -50.0 mV
|
IP3R1
|
|
|
Hs |
Activator (cytosolic Ca2+) |
- |
- |
- |
< 7.5x10-4 |
|
|
⤷ |
Conc range: < 7.5x10-4 M
|
RyR1
|
|
|
Hs |
Antagonist (cytosolic Ca2+) |
Antagonist |
- |
- |
> 1x10-4 |
|
|
⤷ |
Conc range: > 1x10-4 M
|
KNa1.1
|
|
|
Rn |
Gating inhibitor |
Antagonist |
- |
- |
0x100 - 3x10-6 |
20 |
|
⤷ |
Conc range: 0x100 - 3x10-6 M
[20]
|
KCa3.1
|
|
|
Hs |
Activator |
Agonist |
6.1 – 7.0 |
pEC50 |
- |
10,17,21,26,37 |
|
⤷ |
pEC50
6.1 – 7.0
[10,17,21,26,37]
Voltage:
-120.0 – 60.0 mV
|
KCa2.1
|
|
|
Hs |
Activator |
Agonist |
6.2 – 6.5 |
pEC50 |
- |
22,43 |
|
⤷ |
pEC50
6.2 – 6.5
(EC50 6x10-7 – 3x10-7 M)
[22,43]
Voltage:
-80.0 mV
|
KCa2.2
|
|
|
Hs |
Activator |
Agonist |
6.2 – 6.5 |
pEC50 |
- |
7,34,43 |
|
⤷ |
pEC50
6.2 – 6.5
[7,34,43]
|
KCa2.2
|
|
|
Rn |
Activator |
Agonist |
6.1 – 6.4 |
pEC50 |
- |
13,22 |
|
⤷ |
pEC50
6.1 – 6.4
[13,22]
|
KCa2.3
|
|
|
Hs |
Activator |
Agonist |
6.0 – 6.5 |
pEC50 |
- |
15,42-43 |
|
⤷ |
pEC50
6.0 – 6.5
[15,42-43]
|
KCa2.3
|
|
|
Rn |
Activator |
Agonist |
6.2 |
pEC50 |
- |
1 |
|
⤷ |
pEC50
6.2
[1]
|
TRPC5
|
|
|
Hs |
Activator (intracellular Ca2+) |
- |
6.2 |
pEC50 |
- |
|
|
⤷ |
pEC50
6.2
(EC50 6.35x10-7 M)
at negative potentials
|
TRPC5
|
|
|
Mm |
Activator |
Activation |
6.0 |
pEC50 |
- |
2,11 |
|
⤷ |
pEC50
6.0
Internal calcium
[2,11]
|
TRPP1
|
|
|
Hs |
Activator (Intracellular Ca2+) |
- |
6.0 |
pEC50 |
1x10-7 - 1x10-3 |
23 |
|
⤷ |
pEC50
6.0
Conc range: 1x10-7 - 1x10-3 M
[23]
Voltage:
-5.0 mV
|
TRPM5
|
|
|
Mm |
Activator (intracellular Ca2+) |
Agonist |
4.5 – 6.2 |
pEC50 |
- |
14,25,41 |
|
⤷ |
pEC50
4.5 – 6.2
(EC50 3x10-5 – 7x10-7 M)
[14,25,41]
Voltage:
-80.0 – 80.0 mV
|
TRPM4
|
|
|
Hs |
Activator (intracellular Ca2+) |
Agonist |
3.9 – 6.3 |
pEC50 |
- |
30-32,38 |
|
⤷ |
pEC50
3.9 – 6.3
(EC50 1.4x10-4 – 5x10-7 M)
[30-32,38]
Voltage:
-100.0 – 100.0 mV
|
KNa1.1
|
|
|
Mm |
Gating inhibitor |
Antagonist |
6.5 |
pIC50 |
- |
33 |
|
⤷ |
pIC50
6.5
[33]
|
TRPM6
|
|
|
Hs |
Channel blocker |
- |
5.3 – 5.3 |
pIC50 |
- |
|
|
⤷ |
pIC50
5.3 – 5.3
(IC50 5.4x10-6 – 4.8x10-6 M)
inward current mediated by monovalent cations is blocked
|
ZAC
|
|
|
Hs |
Antagonist |
Antagonist |
2.0 |
pIC50 |
- |
40 |
|
⤷ |
pIC50
2.0
[40]
|
TRPC2
|
|
|
N/A |
Activator (Intracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
|
TRPM2
|
|
|
Hs |
Activator (intracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
perhaps via calmodulin
|
CaCC
|
|
|
Hs |
Activator (intracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
|
Cx23
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx25
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx26
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx30
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx30.2
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx30.3
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx31
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx31.1
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx31.9
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx32
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx36
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx37
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx40
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx40.1
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx43
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx45
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx46
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx47
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx50
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx59
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
Cx62
|
|
|
Hs |
Inhibitor (extracellular Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
blocked by raising external Ca2+
|
IP3R2
|
|
|
Hs |
Activator (cytosolic Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
nM range
|
IP3R3
|
|
|
Hs |
Activator (cytosolic Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
nM range
|
RyR1
|
|
|
Hs |
Activator (luminal Ca2+) |
- |
- |
- |
- |
|
|
⤷ |
endogenous
endogenous; μM range
|