TABLE 4

Thermodynamic parameters of binding to the β2-AR, using [3H]MFen as the marker ligand compared with the previously reported parameters obtained using [3H]CGP-12177 as the marker ligand (Jozwiak et al., 2010a)

Distance parameter is the Euclidean distance describing a shift of the (ΔH°; −TΔS°) point, determined in the [3H]MFen experiment with respect to the [3H]CGP-12177-derived point, as illustrated in Fig. 5.

ΔH°TΔS°ΔG°Distance
MFenCGPMFenCGPMFenCGP
kJ/molkJ/molkJ/mol
Propranolol+5.98 ± 0.04−4.5−54.32 ± 0.04−48.95−48.3 ± 0.06−53.511.8
(R)-Isoproterenol+18.4 ± 0.13−18.03−67.9 ± 0.13−19.5−49.5 ± 0.2−37.660.6
(R,R′)-Fen+24.1 ± 0.520−72.6 ± 1.4−38.8−48.5 ± 1.5−38.841.5
(R,S′)-Fen+15.3 ± 3.0+7.1−54.9 ± 1.2−40.0−39.6 ± 3.2−31.117.0
(S,R′)-Fen+18.4 ± 0.13−23.0−47.0 ± 1.1−8.1−32.7 ± 1.6−31.153.9
(S,S′)-Fen+16.2 ± 2.2−35.8−48.5 ± 2.2+6.3−32.2 ± 3.1−29.575.6