Table 3.
pEC50, Emax and pKb values of standard compounds analyzed in the newly developed β-arrestin2 recruitment assay. For comparison, pKi values determined in radioligand displacement studies utilizing homogenates from HEK293T cells stably expressing the wild-type receptors (cf. Table 2) and published data from different assays are included. Data represent means ± SEM from N independent experiments, each performed in triplicate.
| Receptor | cpd | β-Arrestin2 Recruitment | N | Radioligand Displacement | Ref. | |||
|---|---|---|---|---|---|---|---|---|
| pEC50 | Emax [%] | pKb | pKi | |||||
| D2longR | R-(−)-apomorphine | 7.77 ± 0.04 | 87 ± 3 | 4 | 7.48 ± 0.14 | 7.66 [49] | ||
| aripiprazole | 6.65 ± 0.15 | 8 ± 2 | 3 | 8.32 ± 0.02 | 6.84 [50] | |||
| dopamine | 7.24 ± 0.04 | 104 ± 3 | 3 | hi | 7.99 ± 0.16 | 7.05 [55] | ||
| lo | 6.30 ± 0.07 | |||||||
| pramipexole | 8.19 ± 0.05 | 86 ± 4 | 4 | hi | 7.59 ± 0.12 | 8.51 [56] | ||
| lo | 6.00 ± 0.03 | |||||||
| quinpirole | 7.55 ± 0.07 | 100 | 5 | hi | 7.90 ± 0.10 | 7.11 [51] | ||
| lo | 6.11 ± 0.02 | |||||||
| (+)-butaclamol | 8.29 ± 0.10 | 3 | 9.14 ± 0.06 | 8.04 [57] | ||||
| domperidone | 9.13 ± 0.09 | 3 | 9.47 ± 0.07 | 8.87 [58] | ||||
| haloperidol | 8.90 ± 0.05 | 3 | 9.58 ± 0.13 | 8.89 [59] | ||||
| nemonapride | 8.90 ± 0.05 | 3 | 9.76 ± 0.08 | 9.32 [60] | ||||
| S-(−)-sulpiride | 8.86 ± 0.10 | 3 | 7.51 ± 0.09 | 8.22 [61] | ||||
| D3R | R-(−)-apomorphine | 7.43 ± 0.17 | 91 ± 5 | 3 | 8.40 ± 0.03 | 7.93 [49] | ||
| aripiprazole | 7.44 ± 0.05 | 26 ± 1 | 3 | 8.26 ± 0.02 | 7.00 [62] | |||
| dopamine | 7.66 ± 0.14 | 105 ± 8 | 3 | hi | 8.78 ± 0.09 | 7.95 [63] | ||
| lo | 7.23 ± 0.09 | |||||||
| pramipexole | 9.09 ± 0.06 | 99 ± 4 | 4 | 9.18 ± 0.06 | 8.65 [49] | |||
| quinpirole | 8.75 ± 0.07 | 100 | 6 | 8.34 ± 0.07 | 9.07 [56] | |||
| (+)-butaclamol | 7.16 ± 0.17 | −27 ± 9 | 7.35 ± 0.08 | 3/3 | 8.59 ± 0.02 | 7.95 [64] | ||
| domperidone | 8.02 ± 0.14 | −26 ± 4 | 8.06 ± 0.09 | 3/3 | 8.96 ± 0.11 | 8.12 [58] | ||
| haloperidol | 8.29 ± 0.29 | −27 ± 5 | 8.68 ± 0.12 | 3/3 | 8.95 ± 0.03 | 8.70 [65] | ||
| nemonapride | 8.43 ± 0.13 | −25 ± 4 | 9.07 ± 0.12 | 3/3 | 9.99 ± 0.06 | 9.77 [66] | ||
| S-(−)-sulpiride | 8.33 ± 0.10 | −26 ± 8 | 8.23 ± 0.07 | 3/4 | 7.20 ± 0.03 | 7.70 [58] | ||