AUE and EC50 values of entacapone and tolcapone after oral administration of a single dose and repeated doses twice daily for 7 days (dose 10 mg/kg, equivalent to 33 μmol/kg entacapone and 37 μmol/kg tolcapone)
| Entacapone | Tolcapone | |||||
|---|---|---|---|---|---|---|
| AUE | EC50 | AUE | EC50 | |||
| % × h | ng/ml | nM | % × h | ng/ml | nM | |
| Single Dose | ||||||
| Striatum | 146 | –1-a | – | 372 | – | – |
| Duodenum | 466 | 136 | 446 | 667 | 320 | 1170 |
| (−50.0–323) | (−164–1060) | (104–537) | (379–1960) | |||
| Kidney | 571 | 16.6 | 54.2 | 686 | 71.1 | 260 |
| (0.8–32.3) | (2.6–106) | (38.2–104) | (140–381) | |||
| Liver | 450 | 48.1 | 158 | 601 | 161 | 591 |
| (−3.4–99.7) | (−11.0–326) | (81.8–241) | (299–882) | |||
| b.i.d. 7 days | ||||||
| Striatum | 135 | – | – | 334 | – | – |
| Duodenum | 480 | 39.5 | 129 | 676 | 204 | 745 |
| (1.4–77.5) | (4.5–254) | (96.8–311) | (354–1140) | |||
| Kidney | 550 | 13.9 | 45.7 | 717 | 49.4 | 181 |
| (−11.1–39.0) | (−36.5–128) | (26.2–72.6) | (95.8–266) | |||
| Liver | 388 | 67.4 | 221 | 667 | 91.9 | 336 |
| (12.4–122) | (40.7–401) | (63.6–120) | (233–440) | |||
Values were calculated from group data (see Materials and Methods). The EC50 values are best least-squares fit values with the 95% confidence intervals given in parentheses.
↵1-a –, not determined.