Table 3. Potency of NE, DA, clonidine, 7-OH-PIPAT and quinpirole obtained from G protein activation experiments mediated by α2A and α2C adrenoceptors coupled to the different Gαi/o subtypes.
Gα subunit | Receptor | NE | DA | Clonidine | 7-OH-PIPAT | Quinpirole | DA/NE |
---|---|---|---|---|---|---|---|
Gαil | α2A | 11±2** | 170 ± 40 | 3±1 | 80 ± 20 * | 700 ±250 | 15 |
α2C | 90 ±30 | 150 ± 40 | 6±2 | (11 ±4) | ND | 1.7 | |
| |||||||
Gαi2 | α2A | 1.3 ±0.3* | 30 ±3 | 2.0 ±0.8 | 120 ± 6 * | (1000 ±300) | 23 |
α2C | 0.4 ±0.2 | 5±3 | 3±1 | 10 ±2 | (200 ±100) | 12.5 | |
| |||||||
Gαi3 | α2A | 0.6 ±0.2 | 15 ±5 | 1.0 ±0.2 | 60 ± 20 * | (700 ± 400) | 25 |
α2C | 0.4 ±0.2 | 30 ±20 | 4±1 | 5±3 | 400 ±100 | 75 | |
| |||||||
Gαol | α2A | 3.0 ±0.5* | 80 ±10 | 2.0 ± 0.4* | 100 ± 20 | 1300 ± 200** | 27 |
α2C | 19 ±6 | 126 ±8 | (12 ±5) | 20 ±3 | 230 ±50) | 7 | |
| |||||||
Gαo2 | α2A | 6±1* | 100 ± 20 | 4.0 ± 0.2** | 66 ±7* | 820 ± 80 *** | 17 |
α2C | 50 ±10 | 140 ± 20 | 11 ± 2 | 14 ±7 | (100 ±10) | 2.8 |
Potency (EC50 values, in nM) of NE, DA, clonidine and D2-like receptor ligands obtained from G protein activation experiments mediated by α2A and α2C coupled to the different Gαi/o subtypes (Figs. 3 and 4). EC50 values were obtained from a sigmoidal concentration-response function adjusted by nonlinear regression analysis and are expressed as means ± S.E.M. of 3 to 11 experiments performed in triplicate. In parenthesis, values corresponding to experiments showing low efficacy, Emax lower than 50% (Table 4). DA/NE: ratio of EC50 values of DA and NE for each receptor and Gαi/o protein subtype. Statistical differences between α2A and α2C adrenoceptors were calculated by non-paired, two-tailed Student's t test;
p<0.05,
p<0.01 and
p<0.001.