TABLE 1

Affinities of ABT-127 and haloperidol for cloned human hD2L and hD3 receptors

In vitro affinity (Ki, nM) and D2L/D3 selectivity ratio for ABT-127 and haloperidol were determined by inhibition of radioligand binding to cloned human and rat dopamine D2L and D3 receptors. Dopamine D3 receptor binding and dopamine D2L receptor binding were performed with [125I] iodosulpride and [125I] iodospiperone, respectively (for detail sees Material and Methods). All values are mean Ki values (with 95% confidence level) of at least three determinations performed in triplicate.

Receptor SubtypeABT-127Haloperidol
Human D30.98 (0.89–1.08)7.6 (7.3–7.8)
Human D2L145 (130–162)0.56 (0.52–0.59)
D2/D3∼148∼0.07
Rat D32.3 (2.1–2.5)10.4 (9.1–11.9)
Rat D252 (46–58)0.73 (0.68–0.8)
D2/D3∼23∼0.07