| Assay Method Information | |
| | Radioligand Binding Data |
| Description: | The affinities of the synthesized compounds at hD2R and hD3R were tested by radioligand competition binding assays, using the agonist [3H]—(R)-(+)-7-OH-DPAT as radiotracer. Competition against an agonist radioligand allows for a more accurate determination of affinities for novel unlabeled D2-like agonists. Affinities of D2-like agonists and partial agonists, when determined in competition against agonist radioligand probe, reflect the ability of binding the receptors in their “active” state. Well known D3R preferential agonists pramipexole, (+)-PD-128,907 and the diastereomeric mixture of PF592,379 (synthesized as reported in literature) were tested in parallel with the synthesized bitopic analogue compounds, and in the same assay's conditions, to allow a better comparison of affinities and receptor subtype selectivity. |
| Affinity data for this assay | |
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