Table 2.
Transport studies of selenorhodamines 3–10 with MDCK-MDR1 cellsa
Compd | PAB, ×10−9 m s−1 | PBA, ×10−9 m s−1 | PBA/PAB | PPassiveb ×10−9 m s−1 |
---|---|---|---|---|
3c | 1.9 ± 0.5 | 29 ± 3 | 15 | |
(+inh) | 1.7 ± 0.2 | 1.8 ± 0.1 | ~2 | |
4c | 0.9 ± 0.3 | 164 ± 4 | 182 | |
(+inh) | 1.0 ± 0.1 | 11.1 ± 0.2 | ~6 | |
5 | 0.3 ± 0.3 | 18 ± 2 | 57 | |
(+inh) | 0.51 ± 0.3 | 0.57 ± 0.1 | <1 | |
6 | 2.1 ± 0.1 | 78 ± 12 | 37 | |
(+inh) | 0.24 ± 0.1 | 4.8 ± 0.1 | ~2 | |
7 | 0.44 ± 0.1 | 8.8 ± 0.3 | 20 | |
(+inh) | 0.46 ± 0.1 | 0.32 ± 0.2 | <1 | |
8 | 1.4 ± 0.8 | 66 ± 10 | 48 | |
(+inh) | 0.18 ± 0.1 | 2.8 ± 0.2 | ~1 | |
9 | 1.5 ± 1.8 | 6.3 ± 1.2 | 4 | |
(+inh) | 0.51 ± 0.1 | 0.13 ± 0.1 | <1 | |
10 | 1.8 ± 1 | 65 ± 6 | 36 | |
(+inh) | 0.51 ± 0.1 | 4.0 ± 0.7 | ~2 |
Experiments were run with 5 × 10−6 M dye and 4.3 mg mL−1 BSA. Values of transport in the absorptive (PAB) and secretory (PBA) mode in the absence or presence of inhibitor, the ratio PBA/PAB, the % cell associated rhodamine analogue in the absence or presence of inhibitor, and the ratio of cell associated rhodamine in the presence or absence of inhibitor are reported. Details for methods are provided in Section 5. Error limits represent ± SD.
PPassive represents the mean of PAB and PBA in the fully inhibited system.
Data from Ref. 18.