TABLE 1

Responses of a range of β-blockers at the level of cAMP accumulation and CRE-mediated gene transcription (SPAP)

Values represent mean ± S.E.M. of n determinations

cAMP Accumulation CRE-Mediated SPAP Production
β-Blockers log EC50 or IC50Emax (% Basal)a Percentage of Maximum Isoprenaline Responsebn log EC50 or IC50Emax (% Basal)a Percentage of Maximum Isoprenaline Responsebn
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
  • N.R., no response

  • a Maximal response to each β-blocker expressed as a percentage of untreated basal response.

  • b Maximum response to each β-blocker expressed as a percentage of the isoprenaline response determined in the same experiment.