High-affinity and selective dopamine D3 receptor full agonists

We have designed, synthesized and evaluated a series of new compounds with the goal to identify potent and selective D3 ligands. The two most potent and selective new D3 ligands are compounds 38 and 52, which bind to the D3 receptors with a Ki value of <1 nM and display a selectivity of 450-494 times over the D2 receptors and >10,000 times over the D1 receptors. Both 38 and 52 are full agonists with high potency at the D3 receptor in a D3 functional assay.