Table 1.
Functional data of D2R agonists (pEC50 and Emax values) and D2R antagonists (pKb values) from DMR studies at CHO-K1 hD2longR cells. For comparison, functional data (β-arrestin2 recruitment) and binding data (competition binding) of D2R agonists and D2R antagonists are shown from Forster et al.20.
| Compound | DMR | competition bindinga | β-arrestin2 recruitmenta | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| pEC50 | Emax (%) | N | pKb | N | pKiH or pKi | pKiL | pEC50 | Emax (%) | pKb | |
| Quinpirole | 8.48 ± 0.05 | 100 | 9 | – | – | 7.90 ± 0.10a | 6.11 ± 0.02a | 7.55 ± 0.07a | 100a | – |
| Dopamine | 8.17 ± 0.10 | 110 ± 9 | 3 | – | – | 7.99 ± 0.16a | 6.30 ± 0.07a | 7.24 ± 0.04a | 104 ± 3a | – |
| Pramipexole | 8.71 ± 0.08 | 97 ± 0.1 | 3 | – | – | 7.59 ± 0.12a | 6.00 ± 0.03a | 8.19 ± 0.05a | 86 ± 4a | – |
| Aripiprazole | 6.44 ± 0.13 | 62 ± 10 | 3 | – | – | 8.32 ± 0.02a | – | 6.65 ± 0.15a | 8 ± 2a | – |
| R-(−)-apomorphine | 9.25 ± 0.09 | 102 ± 5 | 3 | – | – | 7.48 ± 0.14a | – | 7.77 ± 0.04a | 87 ± 3a | – |
| ( +)-butaclamol | – | – | – | n.d | – | 9.14 ± 0.06a | – | – | – | 8.29 ± 0.10a |
| Domperidone | – | – | – | 9.16 ± 0.20 | 3 | 9.47 ± 0.07a | – | – | – | 9.13 ± 0.09a |
| Haloperidol | – | – | – | 9.17 ± 0.06 | 4 | 9.58 ± 0.13a | – | – | – | 8.90 ± 0.05a |
| Nemonapride | – | – | – | 9.24 ± 0.13 | 3 | 9.76 ± 0.08a | – | – | – | 8.90 ± 0.05a |
| S-(−)-sulpiride | – | – | – | 8.82 ± 0.23 | 3 | 7.51 ± 0.09a | – | – | – | 8.86 ± 0.10a |
Data represent means ± SEM from N or at least three independent experiments, each performed in triplicate. Kb values were derived by converting IC50 values to Kb values according to a modified Cheng-Prusoff equation, as described in “Material and methods”.
n.d. not determined.
aData described in Forster et al.20.