Regulation of the expression of wild-type and mutant H2receptors after prolonged treatment of transfected HEK-293 cells with an agonist or inverse agonist
| H2Receptor | [125I]APT Binding | |
|---|---|---|
| Histamine (1 mM) | Ranitidine (100 μM) | |
| % | ||
| Wild type | 78.3 ± 5.2** | 160.4 ± 26.0* |
| D115A | 224.4 ± 38.0** | 489.8 ± 105.4** |
| R116A | 934.3 ± 150.8*** | 2154.9 ± 334.9*** |
Cells were incubated with the compounds for 24 h, extensively washed, and analyzed for [125I]APT binding. The binding was expressed as the percentage of nontreated cells. Data shown are the mean ± S.E. of three to six independent experiments. The asterisks indicate a significant difference from non-treated cells (seeMaterials and Methods).