Table 1. . KATP channel modulators .
Compound | Structure | Selectivity | IC50/EC50 | Ref. |
---|---|---|---|---|
Inhibitors | ||||
Tolbutamide |
|
SURl >SUR2 |
2–7 μM |
[16,17] |
Glibenclamide (glyburide) |
|
SUR1 >SUR2A |
SUR1 ˜4 nM SUR2A ˜27 nM |
[16] |
Gliclazide |
|
SURl |
˜50 nM |
[18] |
Glipizide |
|
SUR1 |
4 nM |
[19] |
Mitiglinide |
|
SURl ˜ SUR2 |
SUR1 ˜0.3 μM SUR2A ˜0.5 μM |
[20] |
Nateglinide |
|
SUR1 ˜SUR2B >> SUR2A |
SUR1 ˜SUR2B 100 nM SUR2A >1 μM |
[20] |
Activators | ||||
Diazoxide |
|
SURl > SUR2 |
30–60 μM |
[21,22] |
Pinacidil |
|
SUR2 |
˜1 μM |
[21,23] |
P1075 |
|
SUR2 |
≤50 nM |
[21,24] |
Levcromakalim |
|
SUR2 |
-0.4–3 μM |
[21,25] |
NN414 |
|
SUR1 |
450 nM |
[22] |
VU0071063 | SUR1 | ˜7 μM | [26] |