TABLE 1

Binding of epibatidine to desensitized full pentameric receptors containing all mouse subunits The parameters [dissociation constants K1 and K2 and proportion (P) of sites with affinity K1] are derived from fits of eq. 2 to our data and are expressed as mean ± S.E. Data are the mean of three to five experiments.

Wild-Type Subunit Mutant Subunit K1K2P
nM
α2βδγ 0.49 ± 0.04 201 ± 36 0.66 ± 0.03
α2βδ+ γL104Y 0.84 ± 0.09 168 ± 60 0.62 ± 0.04
γS111Y 0.66 ± 0.12 180 ± 18 0.42 ± 0.03
γY117T 1.92 ± 0.04 184 ± 59 0.47 ± 0.05
α2βγ+ δY106L 0.48 ± 0.1 59 ± 6.8 0.55 ± 0.06
δY113S 0.36 ± 0.03 83 ± 11 0.534 ± 0.09
δT119Y 0.61 ± 0.2 71 ± 25 0.58 ± 0.1