TABLE 1

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