Table 3.
D3R over D2R selectivity and Go protein vs. β-arrestin bias factors of bitopic ligands.
| Selectivity (D2R/D3R) | Bias Factors | |||
|---|---|---|---|---|
| Compounds | Go Protein Activation | β-arrestin Recruitment | D3R | D2R |
| Quinpirole | 11.7 | 26.9 | ND | ND |
| rac-FOB02-04 | 3.5 | 11.5 | 0.9 | 1.6 |
| FOB02-04A | 8.1 | 5.8 | 1.4 | 1.4 |
| FOB02-04B | 6.5 | 2.6 | 1.1 | 1.1 |
| AB04-87 | ND | ND | 0.2 | ND |
| AB04-88 | 123.0 | 15.5 | 2.3 | 1.5 |
| rac-AB04-35 | 5.8 | 3.7 | 0.9 | 0.6 |
| AB04-95 | ND | ND | ND | ND |
| AB04-96 | 2.8 | 4.2 | 1.0 | 1.1 |
D3R over D2R selectivity and Go protein versus β-arrestin bias factors are reported. The value > 100 for D3R over D2R selectivity is highlighted in green. Bias factors were calculated as described in Section 2. Bias factor value > 2.0 is highlighted in orange. ND = not determined.