Table 4. Efficacy 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 |
---|---|---|---|---|---|---|
Gαi1 | α2A | 100 ± 5 | 120 ± 6 * | 120 ± 5 | 94 ± 6 | 70 ± 2 * |
α2C | 100 ± 2 | 105 ± 5 | 64 ± 4 ** | 41 ± 1 ** | ND | |
| ||||||
Gαi2 | α2A | 100 ± 10 | 120 ± 20 | 89 ± 6 | 55 ± 2 * | 47 ± 8 * |
α2C | 100 ± 7 | 80 ± 10 | 107 ± 4 | 90 ± 20 | 46 ± 9 ** | |
| ||||||
Gαi3 | α2A | 100 ± 10 | 90 ± 10 | 112 ± 8 | 71 ± 6 | 40 ± 9 ** |
α2C | 100 ± 9 | 95 ± 6 | 85 ± 5 | 90 ± 10 | 80 ± 15 | |
| ||||||
Gαo1 | α2A | 100 ± 7 | 108 ± 6 | 110 ± 10 | 81 ± 9 | 78 ± 9 |
α2C | 100 ± 10 | 100 ± 10 | 41 ± 3 ** | 98 ± 7 | 42 ± 3 ** | |
| ||||||
Gαo2 | α2A | 100 ± 9 | 110 ± 10 | 120 ± 2 | 85 ± 4 | 72 ± 8 |
α2C | 100 ± 8 | 114 ± 6 | 70 ± 8 * | 106 ± 3 | 34 ± 6 ** |
Efficacy (Emax values, as percentage of NE values) 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 (Figures 3 and 4). Emax 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 italics, values of Emax lower than 50%. ND: not detectable. Statistical differences between NE and the other ligands for each receptor and Gαi/o protein subtype were calculated by one-way ANOVA, followed by Dunnett post hoc test;
p<0.05,
p<0.01 and
p <0.001.