Radioligand binding data obtained using COS-7 cell membranes expressing either wild-type H1Rs (WT), or coexpressing both H1R Asp107Ala and H1R Phe432Ala, using either [3H]mepyramine or [3H]-(—)-trans-H2-PAT as a radioligand
Data shown are mean ± S.E.M. of three independent experiments, each performed in triplicate.
[3H]Mepyramine | [3H]-(—)-trans-H2-PAT | |||||
|---|---|---|---|---|---|---|
| Kd | Bmax | Kd | Bmax | |||
| nM | pmol/mg protein | nM | pmol/mg protein | |||
| H1R WT | 1.2 ± 0.1 | 21 ± 4 | 1.2 ± 0.4 | 3.4 ± 1.0 | ||
| H1R Asp107Ala + H1R Phe432Ala | 1.8 ± 0.1 | 0.34 ± 0.1 | 3.0 ± 0.6 | 0.32 ± 0.1 | ||