Table 4.
In vitro plasma protein binding and brain tissue binding of GSK1034702
| Species | Plasma protein binding (%) | f P | Brain tissue binding (%) | f ND |
|---|---|---|---|---|
| Mouse | 48.2 (±1.2) | 0.52 | 86.7 (±0.6) | 0.13 |
| Rat (CD) | 47.2 (±1.4) | 0.53 | 87.7 (±0.5) | 0.12 |
| Rat (LH) | 45.5 (±1.5) | 0.55 | 84.9 (±1.0) | 0.15 |
| Dog | 44.5 (±3.6) | 0.56 | 81.8 (±1.8) | 0.18 |
| Monkey | 41.7 (±2.7) | 0.58 | 83.2 (±1.1) | 0.17 |
| Human | 55.8 (±3.6) | 0.44 | N/A |
Plasma protein binding and brain tissue binding of GSK1034702 evaluated by equilibrium dialysis over 5 h at concentration of 1 μg/mL. Values represent mean ± standard deviation from n = 6 determinations, f P = plasma-free fraction, f ND = brain-free fraction. CD = Sprague Dawley rat and LH = Lister hooded rat.