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.

Chen J, Collins GT, Zhang J, Yang CY, Levant B, Woods J, Wang S.

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

Abstract

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.

PMID:: 18785726; [PubMed - indexed for MEDLINE]
PMCID:: PMC2662387

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Cited by 5 PubMed Central articles

CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist. [ACS Med Chem Lett. 2011]
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Design, synthesis, and evaluation of potent and selective ligands for the dopami...
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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