Inhibition of ABCC4-mediated LTB4 transport in the presence of GSH Membrane vesicles from V79-ABCC4 cells were incubated with 100 nM [3H]LTB4 and 5 mM GSH for 5 min at 37°C with several compounds. Rates of ATP-dependent [3H]LTB4 transport were determined as described and calculated as percentage of control. The rate of [3H]LTB4 transport in the absence of inhibitors amounted to 0.75 ± 0.06 pmol × mg protein-1 in 5 min. Data represent mean values ± S.D. from a triplicate determination.
Compound (+ 5 mM GSH) | Conc. | ATP-Dependent [3H]LTB4 Transport |
|---|---|---|
| μM | % control | |
| [3H]LTB4 (control, 100 nM) | 100 | |
| 5-Hydroxy-6,8,11,14-eicosatetraenoate | 1 | 86 ± 7 |
| 12-Hydroxy-5,8,10,14-eicosatetraenoate | 1 | 106 ± 6 |
| LTC4 | 1 | 39 ± 4 |
| LTD4 | 1 | 67 ± 9 |
| S-Decyl GSH | 10 | 26 ± 3 |
| Sulindac sulfide | 10 | 26 ± 3 |
| Indomethacin | 10 | 32 ± 2 |
| Prostaglandin E2 | 10 | 46 ± 5 |
| Cholyltaurine | 10 | 39 ± 2 |
| Dipyridamole | 10 | 57 ± 3 |
| MK571 | 10 | 60 ± 4 |
| Montelukast | 10 | 52 ± 5 |
| Probenecid | 100 | 73 ± 7 |
| Sulfinpyrazone | 100 | 73 ± 7 |