Table 1.
Comparison of IC50 values obtained for MONIRO‐1 inhibition of L‐, P/Q‐, N‐, R‐ and T‐type calcium channels and the hERG potassium channel, with control compounds Z160/NP118809 and NNC 55‐0396 and other known N‐ and T‐type calcium channel inhibitors
| L‐type (μM) | P/Q‐type (μM) | N‐type (μM) | R‐type (μM) | T‐type (μM) | hERG (μM) | |
|---|---|---|---|---|---|---|
|
Z160/NP118809 (Zamponi et al., 2009) |
12b (Cav1.2) | – | 0.28a | – | – | 7.4b |
| aMONIRO‐1 |
27% @ 100 (Cav1.3) 46% @ 100 (Cav1.2) |
>100 | 34 | >100 |
3.3 (Cav3.1) 1.7 (Cav3.2) 7.2 (Cav3.3) |
>100 |
|
A‐1048400 (Scott et al., 2012) |
28 | 1.3 | 0.8 | – | 0.9 (Cav3.2) | – |
|
Z944 (Tringham et al., 2012) |
32 (Cav1.2) | – | 11 | – |
0.05 (Cav3.1) 0.16 (Cav3.2) |
7.8 |
|
NNC 55–0396 (Chen et al., 2014) |
– | – | – | – |
6.8b (Cav3.1) 96% @10a (Cav3.2) |
– |
|
Ziconotide (Wang et al., 2016) |
– | >10 | 0.18b | – | – | – |
|
TTA‐A2 (Kraus et al., 2010) |
>30b (Cav1.2) | >30b | >30bRecovery from block | >30b |
0.09 (Cav3.1) 0.09 (Cav3.2) |
– |
|
TROX‐1 (Swensen et al., 2012) |
– | 0.29 | 0.19 | 0.28 | – | – |
a
This work.
b
Studies were performed with HEK293 cells stably expressing the desired voltage‐gated calcium channel. –, not tested.