Effects of mutations on the affinity of mianserin and its analogs
Receptors were transiently expressed in HEK 293 cells, and compound affinity for the receptors was determined in competition binding assays using [3H]LSD. Data are expressed as the mean pKi value ± S.E. mean of three separate experiments.
| Compound | Human Wild-Type | Mouse Wild-Type | S175P | Y188F | S277G | S290N |
|---|---|---|---|---|---|---|
| Mianserin | 7.10a ± 0.09 | 8.49 ± 0.08 | 8.34 ± 0.11 | 8.48 ± 0.15 | 8.10 ± 0.12 | 7.59 ± 0.17 |
| BRL-34849 | 6.78 ± 0.06 | 7.62 ± 0.02 | 7.68 ± 0.03 | 7.65 ± 0.02 | 7.51 ± 0.04 | 7.11 ± 0.08 |
| BRL-34969 | 6.39 ± 0.05 | 6.61 ± 0.02 | 6.60 ± 0.06 | 6.67 ± 0.06 | 6.44 ± 0.09 | 6.44 ± 0.09 |
↵ a Affinity of mianserin at the rat wild-type receptor = 7.40.