Ligand | cAMP | pERK1/2 | Ca2+ | Endocytosis | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
pEC50 | Emax | t1/2 | pEC50 | Emax | Peak | pEC50 | Emax | Peak | pEC50 | Emax | t1/2 | |
%ISO | minutes | %ISO | minutes | %ISO | seconds | %ISO | minutes | |||||
ISOa | 8.23 ± 0.15 | 100 | 2.54 ± 0.18 | 7.95 ± 0.13 | 100 | 4 | 7.47 ± 0.21 | 100 | 18.0 ± 1.08 | 7.88 ± 0.26 | 100 | 7.64 ± 0.04 |
EPI | 7.78 ± 0.23 | 74.04 ± 6.19 | 1.64 ± 0.05 | 6.79 ± 0.19 | 157.7 ± 14.13 | 2 | 6.82 ± 0.08 | 112.0 ± 4.10 | 17.4 ± 0.87 | 7.26 ± 0.16 | 115.5 ± 6.24 | 12.26 ± 0.02 |
NE | 7.08 ± 0.25 | 88.32 ± 8.53 | 1.74 ± 0.16 | 6.48 ± 0.12 | 154.6 ± 9.26 | 2 | 6.21 ± 0.24 | 58.01 ± 9.43 | 21.7 ± 1.32 | 5.64 ± 0.30 | 90.00 ± 12.5 | 12.40 ± 0.04 |
SALBa | 9.08 ± 0.31 | 111.3 ± 10.5 | 2.29 ± 0.12 | 10.81 ± 0.28 | 87.16 ± 5.89 | 2 | 7.72 ± 0.28 | 50.93 ± 4.50 | 19.8 ± 0.46 | 5.93 ± 0.31 | 44.94 ± 6.86 | 5.62 ± 0.34 |
SALMa | 8.63 ± 0.20 | 105.5 ± 6.11 | 1.94 ± 0.14 | 10.14 ± 0.23 | 74.39 ± 5.28 | 2 | 5.80 ± 0.39 | 34.45 ± 6.10 | 30.9 ± 2.86 | >4.00 | NR | NR |
LABa | 7.82 ± 0.23 | 51.84 ± 3.73 | 2.61 ± 0.38 | 10.28 ± 0.28 | 111.9 ± 7.52 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
BUCa | 8.64 ± 0.38 | 62.07 ± 7.48 | 2.45 ± 0.16 | 8.51 ± 0.41 | 107.2 ± 22.1 | 2 | >4.00 | NR | NR | >4.00 | NR | NR |
−4.86 ± 0.26 | ||||||||||||
ALP | 9.81 ± 0.39 | 35.76 ± 3.70 | 2.64 ± 0.61 | 9.54 ± 0.28 | 102.3 ± 5.71 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
−6.63 ± 0.34 | ||||||||||||
PINa | 9.50 ± 0.49 | 18.43 ± 2.51 | 0.96 ± 0.14 | 8.90 ± 0.48 | 81.55 ± 19.86 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
−5.76 ± 0.34 | ||||||||||||
XAMa | >4.00 | NR | NR | 6.58 ± 0.22 | 102.7 ± 8.63 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
PRO | >4.00 | NR | NR | 7.87 ± 0.13 | 77.28 ± 7.18 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
−5.79 ± 0.44 | ||||||||||||
CARVa | >4.00 | NR | NR | 7.98 ± 0.12 | 88.55 ± 12.47 | 4 | >4.00 | NR | NR | >4.00 | NR | NR |
−5.68 ± 0.35 | ||||||||||||
ICI | 7.95 ± 0.45 | −35.46 ± 5.39 | 14.15 ± 0.13 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
BIS | 6.96 ± 0.77 | −18.25 ± 5.04 | 6.50 ± 1.01 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
BETa | 6.75 ± 0.42 | −39.80 ± 10.8 | 5.42 ± 2.69 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
MET | 6.87 ± 0.55 | −39.00 ± 9.46 | 6.68 ± 2.46 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
NEB | 7.46 ± 0.57 | −13.79 ± 4.04 | 17.48 ± 3.94 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
NADa | 8.24 ± 0.37 | −34.07 ± 7.80 | 3.48 ± 1.57 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
ATEN | 5.44 ± 0.44 | −49.38 ± 10.9 | 7.77 ± 1.99 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
TIM | 8.81 ± 0.40 | −44.45 ± 5.28 | 4.47 ± 0.11 | >4.00 | NR | NR | >4.00 | NR | NR | >4.00 | NR | NR |
ICI, ICI 118,551; MET, metoprolol; NEB, nebivolol; NR, no response.
↵a Compounds that were selectively signaling via the β2AR.