Table 2.
Comparison of the efficacy D3 dopamine receptor for selective phenylhomopiperazine and phenylpiperazine (WC) analogues.
| ||||
|---|---|---|---|---|
| Compound | Ar | n | Percent Intrinsic Efficacy | |
| %IA D2 | %IAD3 | |||
| WC-10 |
|
n = 1 | 33.5±3.1 | 18.7±2.2 |
| 11b | n = 2 | 61.2±7.3 | 80.3±9.2 | |
|
| ||||
| WC-26 |
|
n = 1 | 29.88±4.8 | 68.7±4.1 |
| 11c | n = 2 | 65.2±7.3 | 67.9±6.7 | |
|
| ||||
| WC-21 |
|
n = 1 | 21.8±2.1 | 47.8±2.2 |
| 11d | n = 2 | 68.2±3.9 | 63.7±9.0 | |
|
| ||||
| WC-44 |
|
n = 1 | 35.3±1.0 | 96.2±4.2 |
| 11e | n = 2 | 57.1±3.4 | 77.8±7.8 | |
|
| ||||
| WC-28 |
|
n = 1 | 26.0±3.0 | 57.2±5.5 |
| 11k | n = 2 | 48.8±11.1 | 64.9±7.2 | |
|
| ||||
| WC-34 |
|
n = 1 | 20.8±4.4 | 62.4±3.3 |
| 11j | n = 2 | 50.8±3.5 | 59.5±12.2 | |
|
| ||||
| WC-23 |
|
n = 1 | 33.4±4.9 | 59.9±0.8 |
| 11q | n = 2 | 84.2±5.5 | 74.5±10.5 | |
The intrinsic efficacy of the test compounds was evaluated by determining the percent inhibition of a forskolin-dependent whole cell adenylyl cyclase assay. The results were normalized to the percent inhibition obtained using the full agonist quinpirole at human D2 (1 μM) and D3 (100 nM) receptors expressed in stably transfected HEK 293 cells. The test drug was used at a concentration equal to approximately 10 × the Ki value that was determined from the radioligand binding analysis. The mean ± the S.E.M. values are reported for n ≥ 3.