TABLE 2
Effects of mutational analysis of the H1R on the functional responses and binding affinities of various ligands compared with the wild-type receptor Receptor affinities (pKd and pKi values) and receptor expression levels (Bmax, pmol/mg of protein) were determined by radioligand-displacement studies using [3H]mepyramine, functional responses were determined using the NF-κ B reporter-gene assay. The pIC50 and pKi values obtained for the mutant H1Rs are presented as the shift (Δ) compared with the values obtained for the wild-type receptor that are indicated in parentheses.