TABLE 2

Stimulation of βarr1 or βarr2 recruitment by antagonists and partial agonists analyzed in the split-luciferase assay

Ligand activities were normalized to (R)-ISO (100%), and statistical significance was determined compared with values from the solvent control (two-way analysis of variance with the Bonferroni post-test).

LigandStimulation βarr1Stimulation βarr2Significance βarr1Significance βarr2
%%
(R)-ISO100.0100.0P < 0.001P < 0.001
Timolol0.220.17P > 0.05P > 0.05
Nadolol0.10−0.02P > 0.05P > 0.05
Labetalol0.160.10P > 0.05P > 0.05
Metoprolol−0.33−0.10P > 0.05P > 0.05
Nebivolol0.090.06P > 0.05P > 0.05
Alprenolol0.09−0.04P > 0.05P > 0.05
Atenolol−0.43−0.30P > 0.05P > 0.05
Sotalol−0.34−0.26P > 0.05P > 0.05
Practolol−0.25−0.01P > 0.05P > 0.05
Bisoprolol−0.07−0.14P > 0.05P > 0.05
Xamoterol−0.25−0.16P > 0.05P > 0.05
Betaxolol−0.19−0.21P > 0.05P > 0.05
(R)-Alprenolol0.140.03P > 0.05P > 0.05
(R)-Propranolol−0.06−0.11P > 0.05P > 0.05
(S)-Propranolol−0.02−0.05P > 0.05P > 0.05
CGP 20712A−0.37−0.25P > 0.05P > 0.05
CGP 20712−0.22−0.06P > 0.05P > 0.05
Pindolol0.400.16P > 0.05P > 0.05
Cyanopindolol0.150.08P > 0.05P > 0.05
Rac-CAR−0.22−0.31P > 0.05P > 0.05
(R)-CAR−0.12−0.18P > 0.05P > 0.05
(S)-CAR−0.001−0.22P > 0.05P > 0.05
ICI 118,551−0.30−0.24P > 0.05P > 0.05
CGP 12177−0.230.06P > 0.05P > 0.05
ICI 215,001−0.63−0.12P < 0.05P > 0.05