Table 1. Potency (pEC50) and intrinsic activity (relative to full agonist) of tested compounds at human cloned α2-adrenoreceptors.
| Compound | α2A-adrenoceptor | α2B-adrenoceptor | ||
|---|---|---|---|---|
| pEC50 | I.A. | pEC50 | I.A. | |
| Brimonidine | 8.1 ± 0.05 | 1 | NT | NT |
| Oxymetazoline | 7.5 ± 0.02 | 0.6 ± 0.04 | 5.5 ± 0.02 | 1 |
| Guanfacine | 7.6 ± 0.03 | 0.8 ± 0.03 | 5.6 ± 0.04 | 0.5 ± 0.04 |
| Clonidine | 5.9 ± 0.03 | 0.7 ± 0.03 | 4.3 ± 0.21 | 0.3 ± 0.05 |
| Yohimbine | 8.3 ± 0.06 | 0—antagonist | 7.8 ± 0.06 | 0—antagonist |
I.A.–intrinsic activity; NT—not tested. pEC50 and I.A. were determined in functional assays (Tango, AequoScreen). Shown is the mean ± SEM (n = 3).