L-745,870 pharmacokinetic parameters in the MPTP-lesioned macaque
The AUC0–24 values were used to calculate the CL. Values are presented as the mean ± S.E.M.
| L-745,870 | ||||
|---|---|---|---|---|
| 0.1 mg/kg p.o. | 0.3 mg/kg p.o. | 1.0 mg/kg p.o. | 0.3 mg/kg i.v. | |
| Cmax, nmol/ml, 0–1 h | 3.4 ± 2.6 | 11.1 ± 9.4 | 97.8 ± 22.8 | 183.8 ± 13.8 |
| Cmax, nmol/ml, 0–2 h | 9.8 ± 3.4 | 27.5 ± 8.6 | 142.7 ± 12.3 | 183.8 ± 13.8 |
| Cmax, nmol/ml, 0–3 h | 10.1 ± 3.2 | 28.4 ± 7.7 | 181.3 ± 5.3 | 183.8 ± 13.8 |
| Cmax, nmol/ml, 0–6 h | 10.1 ± 3.2 | 28.6 ± 7.6 | 181.3 ± 5.3 | 183.8 ± 13.8 |
| Cmax, nmol/ml, 0–8 h | 10.1 ± 3.2 | 28.6 ± 7.6 | 181.3 ± 5.3 | 183.8 ± 13.8 |
| Cmax, nmol/ml, 0–24 h | 10.1 ± 3.2 | 28.6 ± 7.6 | 181.3 ± 5.3 | 183.8 ± 13.8 |
| AUC0–1, h · nmol/ml | 0.8 ± 0.6 | 3.0 ± 2.6 | 55.9 ± 18.8 | 135.2 ± 10.3 |
| AUC0–2, h · nmol/ml | 7.5 ± 3.6 | 22.4 ± 9.7 | 176.1 ± 36.2 | 236.1 ± 21.6 |
| AUC0–3, h · nmol/ml | 16.1 ± 5.9 | 48.8 ± 15.4 | 338.1 ± 42.3 | 307.1 ± 40.4 |
| AUC0–6, h · nmol/ml | 33.3 ± 9.9 | 112.4 ± 28.9 | 700.9 ± 15.4 | 431.6 ± 72.7 |
| AUC0–8, h · nmol/ml | 38.5 ± 11.0 | 142.0 ± 35.6 | 767.1 ± 11.9 | 477.4 ± 79.9 |
| AUC0–24, h · nmol/ml | 50.7 ± 6.1 | 266.9 ± 77.6 | 815.5 ± 51.9 | 648.3 ± 84.2 |
| tmax, h | 2.3 ± 0.3 | 3.3 ± 1.3 | 3.0 ± 0.0 | 0.3 ± 0.1 |
| kel, h−1 | 0.18 ± 0.04 | |||
| t1/2, h | 4.24 ± 1.02 | |||
| CL, l/h | 0.072 ± 0.008 | |||
| Bioavailability, % | 42.0 ± 11.5 | |||