TABLE 3

Log KD values for ICI 118551 (determined from [3H]cAMP accumulation and CRE-luciferase production experiments) and timolol and betaxolol (determined in CRE-luciferase experiments) in the presence of a range of agonists Values are mean ± S.E.M. of n determinations.

Agonist cAMP Accumulation CRE-Luciferase Production
Log KD ICI 118551 n Log KD ICI 118551 n Log KD Betaxolol n Log KD Timolol n
Fenoterol –6.24 ± 0.03 3 –6.04 ± 0.02*** 36 –5.48 ± 0.08 5 –6.86 ± 0.02 5
Terbutaline –6.24 ± 0.09 5 –6.13 ± 0.05*** 4 –5.29 ± 0.04 3 –6.93 ± 0.09 4
Salbutamol –6.30 ± 0.03 3 –6.13 ± 0.06*** 4 –5.28 ± 0.10 3 –6.88 ± 0.05 4
Tulobuterol –6.28 ± 0.06 4 –6.13 ± 0.04*** 4 –5.25 ± 0.00 3 –6.83 ± 0.05 4
Cimaterol –6.33 ± 0.07* 5 –6.09 ± 0.06*** 5 –5.51 ± 0.09 6 –6.87 ± 0.04 6
BRL 37344 –6.13 ± 0.04 3 –5.95 ± 0.02*** 35 –5.54 ± 0.08 5 –6.87 ± 0.08 6
Pronethalol –6.05 ± 0.06 6 N.D. N.D. N.D.
ICI 215001 –6.04 ± 0.08 4 –5.99 ± 0.05 4 –5.41 ± 0.08 5 –6.67 ± 0.04 5
Clenbuterol –6.23 ± 0.06 3 –5.99 ± 0.04 4 –5.17 ± 0.04 3 –6.70 ± 0.04 4
Dobutamine –6.12 ± 0.06 4 –5.97 ± 0.07 4 –5.13 ± 0.00 3 –6.60 ± 0.04 4
CL 316243 –6.08 ± 0.08 5 –5.96 ± 0.11 4 –5.17 ± 0.04 3 –6.72 ± 0.05 4
Salmeterol –6.13 ± 0.06 4 –5.94 ± 0.05 4 –5.33 ± 0.04 3 –6.59 ± 0.10 4
Formoterol –6.21 ± 0.04 3 –5.92 ± 0.08 4 –5.25 ± 0.00 3 –6.77 ± 0.05 4
Noradrenaline –5.83 ± 0.08 5 –5.89 ± 0.04 7 –5.21 ± 0.05 7 –6.57 ± 0.08 8
Adrenaline –5.99 ± 0.03 4 –5.84 ± 0.08 6 –5.24 ± 0.05 6 –6.62 ± 0.08 7
Isoprenaline –5.87 ± 0.05 4 –5.75 ± 0.03 39 –5.17 ± 0.06 6 –6.59 ± 0.06 5
Labetolol –5.53 ± 0.08* 6 –5.47 ± 0.04*** 5 –4.82 ± 0.08** 5 N.D.
Pindolol –5.29 ± 0.05*** 7 –5.24 ± 0.06*** 8 –4.57 ± 0.09*** 7 –5.80 ± 0.07*** 8
CGP 12177 –4.87 ± 0.07*** 5 –5.17 ± 0.04*** 33 –4.78 ± 0.08** 8 –5.81 ± 0.07*** 8
SR 59230A –5.13 ± 0.14*** 6 –5.17 ± 0.04*** 6 –4.24 ± 0.12*** 5 –5.60 ± 0.05*** 4
Alprenolol –5.23 ± 0.06*** 5 –5.14 ± 0.03*** 6 –4.26 ± 0.09*** 5 –5.52 ± 0.09*** 5
Carvedilol –4.79 ± 0.19*** 5 < –5 5 < –4.5 4 < –5 4
  • N.D., not determined.

  • *** , P < 0.001

  • ** , P < 0.01

  • * , P < 0.05 when comparing the log KD value of the antagonist with that obtained in the presence of isoprenaline (one-way analysis of variance, Newman-Keuls post hoc)