TABLE 1.
Drug | Log D | In the absence of PSC-833 (total Papp) |
In the presence of PSC-833 (passive Papp) |
PSC-833-sensitive (active Papp) differenceb |
% of active contribution (BL-AP secretory) | |||||
---|---|---|---|---|---|---|---|---|---|---|
AP-BL absorptive | BL-AP secretorya | Efflux ratio | AP-BL absorptive | BL-AP secretory | Efflux ratio | AP-BL absorptive | BL-AP secretory | |||
CIP | −0.93 | 0.7 ± 0.02 | 2.7 ± 0.07** | 4 | 0.8 ± 0.03 | 0.7 ± 0.01 | 0.9 | 0.1 | 2.0 | 73 |
NOR | −1.16 | 0.6 ± 0.05 | 2.0 ± 0.04* | 3.3 | 0.7 ± 0.03 | 0.6 ± 0.01 | 0.8 | 0.1 | 1.4 | 70 |
LVX | −0.41 | 2.4 ± 0.10 | 6.2 ± 0.12** | 2.6 | 4.2 ± 0.05 | 4.3 ± 0.10 | 1.0 | 1.8 | 1.9 | 30 |
MXF | −0.28 | 5.0 ± 0.20 | 10.4 ± 0.20** | 2.1 | 8.3 ± 0.12 | 7.8 ± 0.09 | 0.9 | 3.3 | 2.6 | 25 |
GRX | 0.03 | 3.1 ± 0.12 | 11.8 ± 0.78** | 3.8 | 7.3 ± 0.26 | 7.2 ± 0.28 | 1.0 | 4.2 | 4.6 | 40 |
PFX | 0.25 | 7.1 ± 0.28 | 9.8 ± 0.19** | 1.4 | 8.7 ± 0.36 | 8.7 ± 0.20 | 1.0 | 1.6 | 1.1 | 11 |
*, P < 0.01, **, P < 0.001.
Calculated as the absolute difference between Papp in the presence and absence of PSC-833. Data are expressed as the means ± SEM of results of three experiments.