Table 1
Pharmacological properties of native and chimeric rat β1- and β3-AR expressed in CHO cells
| Agonist | β1 | β1/β3O3 | β1(β3TM5–6) | β3 | β3/β1O3 | β3(β1TM5–6) |
|---|---|---|---|---|---|---|
| Agonist affinity (pK i ICYP binding) | ||||||
| ISO | 6.6 ± 0.2 | 6.5 ± 0.2 | 5.9 ± 0.03* | 4.9 ± 0.2 | 4.5 ± 0.1 | 5.0 ± 0.2 |
| NE | 5.8 ± 0.3 | 6.0 ± 0.5 | 5.0 ± 0.2* | 4.3 ± 0.1 | 4.1 ± 0.2 | 4.3 ± 0.1 |
| DOB | 5.4 ± 0.2 | 5.4 ± 0.04 | 5.0 ± 0.1 | 4.2 ± 0.1 | 4.2 ± 0.2 | 4.2 ± 0.04 |
| BRL | 5.1 ± 0.1 | 6.4 ± 0.1** | 4.8 ± 0.2 | 7.0 ± 0.1 | 5.7 ± 0.1** | 7.3 ± 0.1 |
| CL | <3.5 | 5.4 ± 0.1** | <3.5 | 6.6 ± 0.3 | 4.5 ± 0.1** | 6.7 ± 0.3 |
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| Agonist potency (pEC50 cAMP accumulation) | ||||||
| ISO | 8.3 ± 0.2 | 7.8 ± 0.4 | 8.6 ± 0.3 | 7.9 ± 0.2 | 8.1 ± 0.2 | 7.9 ± 0.2 |
| NE | 7.0 ± 0.1 | 7.2 ± 0.2 | 7.5 ± 0.2 | 7.4 ± 0.2 | 7.0 ± 0.2 | 7.1 ± 0.4 |
| DOB | 6.5 ± 0.4 | 6.1 ± 0.5 | 6.0 ± 0.5 | 5.6 ± 0.3 | 5.5 ± 0.1 | 5.5 ± 0.4 |
| BRL | 5.9 ± 0.3 | 7.9 ± 0.3** | 5.2 ± 0.3 | 9.7 ± 0.1 | 6.9 ± 0.2** | 8.7 ± 0.1* |
| CL | <3.5 | 6.9 ± 0.4** | <3.5 | 9.8 ± 0.05 | 5.7 ± 0.1** | 9.2 ± 0.4 |
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* p < .05, ** p < .01 versus native β-AR.