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

Jianyong Chen, Gregory T. Collins, Jian Zhang, Chao Yie Yang, Beth Levant, James Woods, Shaomeng Wang

Research output: Contribution to journalArticle

27 Scopus citations

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 Ki value of 0.41 nM to D3 and a selectivity of > 30000- and 800-fold over the D1-like and D 2 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.

Original languageEnglish (US)
Pages (from-to)5905-5908
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number19
DOIs
StatePublished - Oct 9 2008
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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