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 EC150 |
Log EC250 |
Site 1 |
Iso Maximum |
n | |
---|---|---|---|---|---|
% | % | ||||
3H-cAMP accumulation | |||||
Cyanopindolol | −10.25 ± 0.02 | −7.31 ± 0.09 | 64.8 ± 2.4 | 31.8 ± 1.1 | 4 |
7-Methylcyanopindolol | −9.76 ± 0.14 | 2.3 ± 0.3 | 4 | ||
Carazolol | −9.95 ± 0.10 | −6.76 ± 0.06 | 40.2 ± 1.2 | 22.4 ± 0.9 | 4 |
ICI118551 | No response | 4 | |||
CRE-SPAP production | |||||
Cyanopindolol | −10.22 ± 0.06 | −7.19 ± 0.22 | 56.1 ± 5.2 | 40.2 ± 2.4 | 8 |
7-Methylcyanopindolol | No response | 8 | |||
Carazolol | −9.74 ± 0.22 | −6.66 ± 0.25 | 28.7 ± 3.2 | 31.8 ± 3.2 | 4 |
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.