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J Med Chem. 2008 Oct 9;51(19):5905-8. doi: 10.1021/jm800471h. Epub 2008 Sep 12.

Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile.

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  • 1Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, USA.


A series of compounds structurally related to pramipexole were designed, synthesized, and evaluated as ligands for the dopamine 3 (D3) receptor. Compound 12 has a K(i) value of 0.41 nM to D3 and a selectivity of >30000- and 800-fold over the D1-like and D2 receptors, respectively. Our in vivo functional assays showed that this compound is a partial agonist at the D3 receptor with no detectable activity at the D2 receptor.

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