Ligand | Affinity | Adenylate Cyclase | Internalization Intrinsic Activity | ||||
---|---|---|---|---|---|---|---|
K0.5 | nH | KD(High) (nM) RHigh (%) | KD(Low) (nM) RLow (%) | EC50 | Intrinsic Activity | ||
nM | nM | ||||||
Dopamine | 300 ± 120 | -0.45 ± 0.04 | 19 ± 0.30 | 2100 ± 38 | 23 ± 18 | ||
46 ± 3.0 | 44 ± 3.0 | ||||||
Apomorphine | 240 ± 76 | -0.85 ± 0.04 | 0.49 ± 0.03 | 240 ± 2.0 | 37 ± 3 | 86 ± 4 | 0.0 |
7.6 ± 2.0 | 92 ± 2.0 | ||||||
Dinapsoline | 48 ± 5.0 | -0.46 ± 0.05 | 1.4 ± 0.03 | 140 ± 3.6 | 4.0 ± 3.0 | 100 ± 18 | 106 ± 3 |
43 ± 6.0 | 57 ± 6.0 | ||||||
Dinoxyline | 16 ± 9.3 | -0.40 ± 0.05 | 0.12 ± 0.01 | 30 ± 0.46 | 4.0 ± 3.0 | 102 ± 14 | 118 ± 2 |
44 ± 4.0 | 56 ± 4.0 | ||||||
Dihydrexidine | 71 ± 8.5 | -0.63 ± 0.09 | 0.06 ± 0.01 | 25 ± 0.20 | 15 ± 0.5 | 96 ± 8 | 110 ± 5 |
21 ± 3.0 | 79 ± 3.0 | ||||||
A86929 | 7.8 ± 1.5 | -0.68 ± 0.06 | 2.5 ± 0.03 | 110 ± 4.2 | 2.3 ± 0.5 | 91 ± 15 | 108 ± 3 |
68 ± 7.0 | 32 ± 7.0 | ||||||
SKF38393 | 240 ± 140 | -0.63 ± 0.05 | 14 ± 0.39 | 370 ± 11 | 13 ± 1.0 | 67 ± 1 | 0.0 |
48 ± 11 | 52 ± 11 | ||||||
SKF77434 | 52 ± 2 | -0.75 ± 0.07 | 0.79 ± 0.04 | 45 ± 0.63 | 11 ± 2.0 | 46 ± 12 | 0.0 |
18 ± 6.0 | 82 ± 6.0 | ||||||
SKF83959 | 2.7 ± 0.7 | -0.94 ± 0.10 | N.A. | N.A. | 5.6 ± 0.6 | 42 ± 3 | 0.0 |
SKF82957 | 2.5 ± 0.3 | -1.00 ± 0.09 | N.A. | N.A. | 0.8 ± 0.6 | 55 ± 9 | 0.0 |
SKF81297 | 10 ± 1 | -0.654 ± 0.05 | 1.8 ± 0.12 | 36 ± 0.59 | 2.6 ± 1.2 | 89 ± 11 | 105 ± 3 |
42 ± 8.0 | 58 ± 8.0 | ||||||
SKF82958 | 6.5 ± 0.2 | -0.73 ± 0.05 | 1.2 ± 0.03 | 14 ± 0.31 | 3.0 ± 2.6 | 86 ± 12 | 105 ± 3 |
46 ± 14 | 54 ± 14 | ||||||
A77636 | 3.8 ± 1.3 | -1.01 ± 0.07 | N.A. | N.A. | 5.3 ± 2.0 | 99 ± 7 | 118 ± 2 |
A68930 | 2.4 ± 0.2 | -0.78 ± 0.05 | 0.90 ± 0.01 | 18 ± 0.49 | 0.3 ± 0.1 | 97 ± 3 | 124 ± 2 |
73 ± 0.07 | 27 ± 0.02 |
N.A., not applicable (nH = 1).