CJ-1639: A potent and highly selective dopamine D3 receptor full agonist

Jianyong Chen, Gregory T. Collins, Beth Levant, James Woods, Jeffrey R. Deschamps, Shaomeng Wang

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

We have identified several ligands with high binding affinities to the dopamine D3 receptor and excellent selectivity over the D2 and D1 receptors. CJ-1639 (17) binds to the D3 receptor with a K i value of 0.50 nM and displays a selectivity of >5000 times over D2 and D1 receptors in binding assays using dopamine receptors expressed in the native rat brain tissues. CJ-1639 binds to human D3 receptor with a K i value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 receptors. CJ-1639 is active at 0.01 mg/kg at the dopamine D3 receptor in the rat and only starts to show a modest D2 activity at doses as high as 10 mg/kg. CJ-1639 is the most potent and selective D3 full agonist reported to date.

Original languageEnglish (US)
Pages (from-to)620-625
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume2
Issue number8
DOIs
StatePublished - Aug 11 2011
Externally publishedYes

Keywords

  • Dopamine receptors
  • agonists
  • drug abuse
  • ligands

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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