Table 2.
IC50 Values of Antipsychotics for Ionic Currents/Channels
Compound | Model system | Potassium channels/currents
|
Calcium channels/current
|
Sodium channels/currents INa | References | |||
---|---|---|---|---|---|---|---|---|
KV/delayed rectifier IKr | Transient outward Ito | Inward rectifier IK1 | HERG | ICaL | ||||
Chlorpromazine | CHO | 1.47 μM | 157 | |||||
| ||||||||
Clozapine | HEK-293 | >50 μM | 320 nM | 29 μM | 148 | |||
| ||||||||
Droperidol | Ventricular myocytes HEK-293 | 28 nM | 32.2 μM | 145 | ||||
| ||||||||
Fluspirilene | Xenopus oocytes | 2.34 μM | 150 | |||||
| ||||||||
Haloperidol | PC12 cells | 20 μM | 164 | |||||
Ventricular myocytes | 5 μM | 81 | ||||||
HEK-293 | >10 μM | >100 μM | 26.8 nM | 14.4 μM | 148 | |||
20 nM | 165 | |||||||
Xenopus oocytes | 1.36 μM | 150 | ||||||
Xenopus oocytes | 1.0 μM | 146 | ||||||
| ||||||||
Olanzapine | HEK-293 | >100 μM | >100 μM | 731 nM | >100 μM | 148 | ||
CHO | 6013 nM | 147 | ||||||
| ||||||||
Pimozide | HEK-293 | >100 μM | >100 μM | 54.6 nM | 21.9 μM | 148 | ||
Xenopus oocytes | 1.74 μM | 150 | ||||||
CHO | 18 nM | 154 | ||||||
| ||||||||
Quetiapine | CHO | 5765 nM | 147 | |||||
| ||||||||
Risperidone | canine ventricular myocytes | 0.92 μM | 151 | |||||
HEK-293 | >100 μM | >100 μM | 148 nM | >50 μM | 148 | |||
CHO | 167 nM | 147 | ||||||
CHO | 261 nM | 155 | ||||||
| ||||||||
Sertindole | HEK-293 | >10 μM | >10 μM | 14 nM | >10 μM | 148 | ||
HEK-293 | 21 μM | 14.7 nM | 153 | |||||
CHO | 3 nM | 147 | ||||||
| ||||||||
Thioridazine | Ventricular myocytes | 1.25 μM | 149 | |||||
tsA201 | ||||||||
CHO | 1.25 μM | |||||||
CHO | 1.07 μM | 158 | ||||||
HEK-293 | 91 nM | 147 | ||||||
27 μM | 33.2 nM | 7 μM | 148 | |||||
| ||||||||
Ziprasidone | HEK-293 | >10 μM | > 10 μM | 125 nM | >10 μM | 148 | ||
CHO | 169 nM | 147 |
CHO =Chinese hamster ovary cells; PC12 cells=rat pheochromocytoma cells; HEK-293= Human embryonic kidney cells.