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 journalArticle

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

Fingerprint Dive into the research topics of 'CJ-1639: A potent and highly selective dopamine D3 receptor full agonist'. Together they form a unique fingerprint.

  • Cite this