Table 1. Log KD values obtained from 3H-CGP 12177 whole cell binding studies at the three turkey β-adrenoceptors.
tβtrunc | tβ3C | tβ4C | Human β1 | Human β2 | Human β3 | ||||
Acebutolol | −5.85±0.02 | 6 | −5.39±0.09 | 10 | −5.41±0.08 | 6 | −6.46 | −6.08 | −4.41 |
Adrenaline | −6.01±0.04 | 6 | −5.81±0.06 | 9 | −5.77±0.08 | 7 | −5.15 | −6.13 | −4.70 |
Alprenolol | −7.96±0.04 | 5 | −8.44±0.10 | 7 | −7.85±0.10 | 7 | −7.83 | −9.04 | −6.93 |
Atenolol | −5.40±0.06 | 6 | −4.75±0.10 | 10 | −4.76±0.05 | 7 | −6.66 | −5.99 | −4.11 |
Betaxalol | −6.90±0.04 | 6 | −6.29±0.08 | 8 | −6.24±0.06 | 7 | −8.21 | −7.38 | −5.97 |
BRL35135A | −6.32±0.07 | 5 | −7.42±0.06 | 5 | −6.39±0.03 | 5 | −6.08 | −7.38 | −6.73 |
BRL37344 | −5.19±0.03 | 6 | −6.28±0.06 | 7 | −5.89±0.10 | 7 | −5.19 | −6.51 | −6.45 |
Bisoprolol | −6.70±0.03 | 6 | −5.58±0.08 | 6 | −6.26±0.08 | 7 | −7.83 | −6.70 | −5.67 |
Bupranolol | −8.43±0.04 | 6 | −9.07±0.07 | 7 | −8.18±0.09 | 7 | −8.51 | −9.85 | −7.04 |
Bucindolol | −9.43±0.06 | 7 | −9.72±0.09 | 9 | −9.41±0.07 | 6 | −9.31 | −9.99 | −8.04 |
Butoxamine | −5.24±0.03 | 6 | −5.99±0.08 | 6 | −4.90±0.05 | 4 | −4.85 | −6.23 | >−4 |
Carazolol | −10.20±0.05 | 6 | −10.92±0.11 | 6 | −10.27±0.09 | 6 | −9.69 | −10.49 | −8.35 |
Carvedilol | −9.43±0.05 | 5 | −9.58±0.07 | 7 | −9.91±0.02 | 7 | −8.75 | −9.40 | −8.30 |
CGP20712A | −7.53±0.04 | 8 | −5.40±0.11 | 9 | −6.05±0.07 | 12 | −8.81 | −6.11 | −5.19 |
Cimaterol | −7.17±0.03 | 9 | −7.06±0.08 | 8 | −6.75±0.04 | 8 | −6.57 | −7.26 | −5.28 |
CL316243 | >−4 | 6 | >−4 | 4 | >−4 | 4 | >−3 | −4.10 | −5.11 |
Clenbuterol | −6.74±0.07 | 6 | −7.38±0.10 | 7 | −6.44±0.03 | 7 | −6.62 | −7.90 | −5.35 |
S-Cyanopindolol | −10.89±0.06 | 6 | −11.37±0.07 | 6 | −10.81±0.09 | 6 | −10.39 | −11.09 | −8.36 |
Denopamine | −6.29±0.05 | 7 | −5.63±0.06 | 6 | −5.95±0.03 | 6 | −6.12 | −5.83 | −5.30 |
Dobutamine | −5.69±0.03 | 6 | −5.57±0.06 | 8 | −6.00±0.06 | 7 | −5.23 | −5.84 | −5.09 |
Fenoterol | −6.36±0.03 | 6 | −6.69±0.07 | 10 | −6.22±0.10 | 10 | −5.04 | −7.03 | −5.39 |
Formoterol | −7.33±0.06 | 6 | −7.96±0.07 | 7 | −7.70±0.07 | 7 | −6.11 | −8.63 | −5.82 |
ICI118551 | −7.20±0.03 | 5 | −8.93±0.06 | 9 | −7.37±0.03 | 9 | −6.52 | −9.26 | −6.44 |
ICI215001 | −5.79±0.05 | 6 | −5.31±0.09 | 7 | −6.55±0.06 | 10 | −6.37 | −5.86 | −6.63 |
Isoprenaline | −6.86±0.08 | 7 | −6.50±0.08 | 7 | −6.71±0.09 | 7 | −6.06 | −6.64 | −5.52 |
Labetolol | −7.51±0.05 | 6 | −7.42±0.04 | 7 | −7.70±0.04 | 6 | −7.63 | −8.03 | −6.18 |
L755507 | −7.17±0.03 | 7 | −6.56±0.06 | 5 | −7.63±0.11 | 5 | −6.23 | −6.83 | −8.60* |
Metaproterenol | −5.64±0.07 | 6 | −5.38±0.09 | 5 | −5.13±0.09 | 6 | −4.71 | −5.30 | −4.06 |
Metoprolol | −6.42±0.03 | 7 | −5.96±0.09 | 6 | −5.78±0.07 | 7 | −7.26 | −6.89 | −5.16 |
Nadolol | −7.99±0.04 | 6 | −7.95±0.09 | 6 | −7.74±0.03 | 6 | −7.23 | −8.60 | −6.18 |
Noradrenaline | −6.60±0.03 | 6 | −4.94±0.07 | 7 | −6.30±0.08 | 7 | −5.74 | −5.41 | −5.53 |
Nebivolol | −8.25±0.05 | 6 | −7.78±0.09 | 8 | −8.83±0.08 | 9 | −9.06 | −7.92 | −7.04 |
Pindolol | −8.55±0.03 | 6 | −8.71±0.10 | 8 | −8.28±0.06 | 7 | −8.57 | −9.23 | −7.08 |
Pronethalol | −6.85±0.01 | 6 | −6.99±0.07 | 7 | −7.06±0.04 | 7 | −6.44 | −7.36 | −5.89 |
Propranolol | −8.51±0.05 | 7 | −8.49±0.06 | 7 | −8.51±0.06 | 7 | −8.16 | −9.08 | −6.93 |
Ractopamine | −6.75±0.03 | 6 | −6.65±0.04 | 6 | −6.57±0.04 | 6 | −6.97 | −6.93 | −5.82 |
Salbutamol | −4.99±0.03 | 6 | −6.14±0.07 | 7 | −5.36±0.05 | 7 | −4.66 | −6.12 | −4.33 |
Salmeterol | −5.92±0.04 | 8 | −8.50±0.07 | 8 | −7.09±0.04 | 8 | −5.73 | −9.26 | −6.33 |
SDZ21009 | −9.27±0.08 | 6 | −10.17±0.08 | 10 | −9.06±0.07 | 7 | −8.94 | −10.28 | −7.10 |
SR59230A | −7.39±0.04 | 7 | −7.96±0.08 | 6 | −7.65±0.06 | 7 | −7.54 | −8.45 | −7.37 |
Sotalol | −6.14±0.06 | 6 | −6.27±0.08 | 6 | −6.16±0.05 | 7 | −5.77 | −6.85 | −5.05 |
Terbutaline | −4.61±0.04 | 6 | −5.62±0.09 | 10 | −4.47±0.05 | 5 | −3.82 | −5.62 | −3.90 |
Timolol | −8.76±0.02 | 5 | −9.24±0.10 | 11 | −8.70±0.06 | 7 | −8.27 | −9.68 | −6.80 |
Tulobuterol | −5.60±0.06 | 7 | −6.64±0.08 | 9 | −5.46±0.04 | 7 | −5.62 | −6.83 | −4.72 |
Xamoterol | −6.58±0.02 | 6 | −5.64±0.09 | 8 | −6.23±0.05 | 7 | −7.22 | −6.07 | −4.45 |
ZD2079 | −3.77±0.03 | 4 | >−4 | 4 | >−4 | 4 | −4.21 | >−4 | −4.59 |
ZD7114 | −7.30±0.09 | 6 | −6.59±0.10 | 7 | −7.59±0.04 | 7 | −7.58 | −7.31 | −6.78 |
zinterol | −6.40±0.03 | 6 | −7.62±0.08 | 6 | −6.80±0.03 | 6 | −5.96 | −8.04 | −6.27 |
Log KD values obtained from 3H-CGP 12177 whole cell binding studies in CHO cells stably expressing either the tβtrunc, tβ3C or tβ4C adrenoceptors. The human β1 β2 and β3-data is taken from [25] and [30] and is given for comparison. Values represent mean ± s.e.m. for n separate experiments.
*binding to site 1 [30].