Ki of various compounds in inhibiting TEA uptake mediated by hOCT1, rOCT1 and hOCT2
| Compounds | Ki | ||
|---|---|---|---|
| hOCT12-a | rOCT12-b | hOCT22-c | |
| μM | |||
| TEA | 161 | 952-d | 762-d |
| MPP+ | 12.3 | 132-d | 2.4 |
| Decynium-22 | 2.73 | 0.36 | 0.1 |
| Tetrapentylammonium | 7.46 | 0.43 | 1.5 |
| Procainamide | 73.9 | 13 | 50 |
| Desipramine | 5.36 | 2.8 | 16 |
| NMN | 7,700 | 1,000 | 266 |
| Quinine | 22.9 | 4.3 | 3.4 |
| Quinidine | 17.5 | 6.0 | – |
| Corticosterone | 7.02 | 72 | – |
| Clonidine | 0.55 | 1.4 | – |
| Vecuronium | 232 | 4.32-e | – |
| Cimetidine | 166 | – | – |
| Midazolam | 3.70 | – | – |
| (±)-Verapamil | 2.90 | – | – |
| Acebutolol | 95.8 | – | – |
↵2-a Data obtained from the present study in transfected HeLa cells. The coefficient of variation values ranged from 3.29% for vecuronium to 83.3% for midazolam.
↵2-b Data obtained from the references (Grundemann et al., 1994, 1997; Martel et al., 1996). Studies were conducted in either oocytes or transfected HEK-293 cells.
↵2-c Data obtained from the reference (Gorboulev et al., 1997). Studies were conducted in oocytes.
↵2-d Km values.
↵2-e Unpublished data from this laboratory.