TABLE 2

CRE-SPAP gene transcription response and 3H-cAMP accumulation in ligand-stimulated tβ1AR-CHO cell lines

Cyanopindolol and carazolol stimulated concentration responses that were best described by a two-component curve. Here, the log EC50 values are given for each component. The percentage of the response represented by the first component and the percentage of the total response in relation to the isoprenaline stimulation are given. Values represent the mean ± S.E.M. of n separate experiments.

Log EC150Log EC250Site 1Iso Maximumn
%%
3H-cAMP accumulation
 Cyanopindolol−10.25 ± 0.02−7.31 ± 0.0964.8 ± 2.431.8 ± 1.14
 7-Methylcyanopindolol−9.76 ± 0.142.3 ± 0.34
 Carazolol−9.95 ± 0.10−6.76 ± 0.0640.2 ± 1.222.4 ± 0.94
 ICI118551No response4
CRE-SPAP production
 Cyanopindolol−10.22 ± 0.06−7.19 ± 0.2256.1 ± 5.240.2 ± 2.48
 7-MethylcyanopindololNo response8
 Carazolol−9.74 ± 0.22−6.66 ± 0.2528.7 ± 3.231.8 ± 3.24
  • ICI118551, (–)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)-amino]-2-butanol. Iso Max, maximum response compared to the response of isoprenaline.