Table 1.
D2long | D3 | D4 | D2:D3 Ratio | %IA D2 | %IA D3 |
---|---|---|---|---|---|
0.22 ± 0.01 nM | 13.1 ± 2.3 nM | 212 ± 45 nM | 60 | 61.2 ± 4.4 | 52.5 ± 4.4 |
Ki values (nM) were determined using human receptors expressed in HEK cells with 125I-IABN. The Ki values represent the mean values for n > 3 determinations.
Percent intrinsic activity (%IA) at human D2 or D3 receptors was determined using a forskolin-dependent adenylyl cyclase whole cell assay at a concentration of test compound >10 × Ki value. The mean values (n > 3) were normalized to values obtained using the full agonist quinpirole.