Table 2

Binding parameters of 125I-cyanopindolol, [3H]propranolol, and [3H]ICI 118551 derived from saturation experiments carried out in membranes expressing the β2AR alone or in combination with Gαsβ1γ2

LigandnKdBmax
β2ARβ2AR/αsβ1γ2β2ARβ2AR/αsβ1γ2
pmol/mg protein
Cyanopindolol494  ± 19 pM84  ± 23 pM18  ± 2.1511  ± 0.392-a
Propranolol30.9  ± 0.31 nM0.7  ± 0.26 nM14  ± 0.568.6  ± 1.002-b
ICI 11855141.3  ± 0.17 nM1.3  ± 0.37 nM17  ± 1.788.4  ± 1.402-b

K d and B max were determined as described under Materials and Methods. Data were analyzed using the curve-fitting software GraphPad-Prism. Values represent means ± S.E.M. of n independent experiments performed in triplicates.

    • 2-a  p < 0.05.

    • 2-b  p < 0.01.