Table 2. Permeability (Papp) of VMY-2-95 Across Caco-2 Cell Monolayers.a.
| drug transport Papp (× 10–6 cm/sec) |
|||
|---|---|---|---|
| compound (concentration) | A → B | B → A | efflux ratio |
| VMY-2-95·2HCl (100 μM) | 21.1 ± 0.02 | 23.4 ± 0.02 | 1.11 |
| VMY-2-95·2HCl (100 μM) + verapamil (100 μM) | 20.2 ± 0.02 | 20.7 ± 0.02 | 1.02 |
| VMY-2-95·2HCl (100 μM) + MK-571 (100 μM) | 23.0 ± 0.27 | 26.9 ± 0.32 | 1.17 |
a
Bidirectional transport of VMY-2-95 was observed across Caco-2 cell monolayers for 2 h in the absence and presence of 100 μM P-gp inhibitor, verapamil, or 100 μM MRP1/MRP2 inhibitor, MK-571. Data are mean ± SD (n = 3). Efflux ratio = PappB–A/PappA–B.