cAMP Accumulation | CRE-Mediated SPAP Production | |||||||
---|---|---|---|---|---|---|---|---|
β-Blockers | log EC50 or IC50 | Emax (% Basal)a | Percentage of Maximum Isoprenaline Responseb | n | log EC50 or IC50 | Emax (% Basal)a | Percentage of Maximum Isoprenaline Responseb | n |
Agonists | ||||||||
Labetolol | −8.08 ± 0.02 | 448.8 ± 46.7 | 8.5 ± 0.6 | 12 | −8.76 ± 0.04 | 371.6 ± 27.3 | 66.9 ± 5.2 | 14 |
Acebutolol | −6.01 ± 0.06 | 295.2 ± 36.0 | 3.8 ± 0.6 | 4 | −6.41 ± 0.06 | 315.0 ± 25.9 | 54.1 ± 1.9 | 11 |
Pindolol | −8.96 ± 0.06 | 252.1 ± 7.7 | 3.3 ± 0.5 | 4 | −9.39 ± 0.07 | 329.6 ± 23.9 | 54.1 ± 2.6 | 11 |
Alprenolol | −9.08 ± 0.04 | 201.3 ± 10.4 | 3.0 ± 0.7 | 12 | −9.42 ± 0.03 | 310.8 ± 8.7 | 48.5 ± 1.4 | 28 |
Carvedilol | −9.10 ± 0.08 | 194.7 ± 10.6 | 1.0 ± 0.04 | 6 | −9.32 ± 0.15 | 208.2 ± 10.8 | 20.7 ± 1.3 | 11 |
CGP 20712A | N.R. | 8 | −5.90 ± 0.17 | 142.5 ± 5.4 | 12.3 ± 1.4 | 8 | ||
Inverse agonists | ||||||||
Timolol | −8.89 ± 0.09 | 72.1 ± 4.5 | 5 | N.R. | 9 | |||
Bisoprolol | −6.70 ± 0.13 | 71.0 ± 6.1 | 4 | N.R. | 13 | |||
Metoprolol | −7.22 ± 0.21 | 70.4 ± 6.2 | 6 | N.R. | 6 | |||
Sotalol | −6.79 ± 0.12 | 47.0 ± 6.0 | 4 | N.R. | 8 | |||
Bupranolol | −9.55 ± 0.07 | 25.3 ± 1.0 | 4 | N.R. | 7 | |||
Atenolol | −6.63 ± 0.33 | 55.1 ± 7.7 | 5 | −6.49 ± 0.16 | 84.1 ± 4.6 | 4 | ||
ICI 118551 | −9.08 ± 0.18 | 36.1 ± 4.4 | 8 | −9.62 ± 0.13 | 85.6 ± 2.7 | 9 | ||
Propranolol | ||||||||
(±)-Propranolol | −9.17 ± 0.08 | 54.2 ± 7.3 | 7 | −9.40 ± 0.05 | 154.9 ± 3.5 | 14.2 ± 0.9 | 25 | |
R(+)-Propranolol | −7.31 ± 0.04 | 34.12 ± 0.74 | 3 | −7.74 ± 0.34 | 179.0 ± 15.9 | 13.5 ± 0.9 | 4 | |
S(−)-Propranolol | −9.19 ± 0.05 | 32.0 ± 2.14 | 3 | −9.54 ± 0.10 | 176.3 ± 16.7 | 11.4 ± 1.3 | 3 |