Table 2.
VX-765 and VRT-043198 are detected in the brain after a single IP dose of VX-765.
| Time (h) | Mouse 1 VX-765 (μM) | Mouse 2 VX-765 (μM) | Mouse 1 VRT-043198 (μM) | Mouse 2 VRT-043198 (μM) | Mean VX-765 (μM)(a) | Mean VRT-043198 (μM)(b) |
|---|---|---|---|---|---|---|
| 0.25 | 0.24 | 0.07 | 2.54 | 0.85 | 0.16 | 1.70 |
| 0.50 | 0.05 | 0.09 | 0.59 | 0.65 | 0.07 | 0.62 |
| 1 | NQ | NQ | 0.21 | 0.27 | − | 0.24 |
| 3 | NQ | NQ | 0.08 | NQ | − | 0.08 |
| 6 | NQ | NQ | NQ | NQ | − | − |
| 8 | NQ | NQ | NQ | NQ | − | − |
| 24 | NQ | NQ | NQ | NQ | − | − |
| Cmax (μM)(c) | 0.24 | 0.09 | 2.54 | 0.85 | 0.16 | 1.70 |
| Tmax (h)(d) | 0.25 | 0.50 | 0.25 | 0.25 | 0.38 | 0.25 |
| Half-life (t1/2) (h)(e) | NC | NC | 0.99 | NR | − | 0.99 |
| MRTinf (h)(f) | NC | NC | 0.98 | 0.76 | − | 0.87 |
NQ: not quantifiable. No peak of below lower limit of quantification: 0.025 μM for VX-765 and 0.049 μM for VRT-043198.
NC: not calculated. Not enough data points.
NR: not reported. The span of the terminal phase is too short to allow for accurate estimation of half-life.
Individual data points showing VX-765 and VRT-043198 brain concentrations up to 24 h post-injection (n = 2 per time point). (a) VX-765 and (b) VRT-043198 mean concentrations at each time point. (c) Maximum concentration achieved (Cmax), (d) time to reach Cmax (Tmax), (e) half-life (t1/2) and (f) mean residence time (MRT) in the brain for VX-765 and VRT-043198.