Further SAR study on 11-O-substituted aporphine analogues: Identification of highly potent dopamine D3 receptor ligands

Na Ye, Qianqian Wu, Liyuan Zhu, Longtai Zheng, Bo Gao, Xuechu Zhen, Ao Zhang

Research output: Contribution to journalArticle

17 Scopus citations


A series of new aporphine analogues (aporlogues) were prepared from appropriate aporphine precursors and arylpiperazines using the Click reaction protocol. These compounds displayed good to high affinity at the D3 receptor, low or no affinity at the D1 and D2 receptors. Compounds 7f and 11c stood out as the most potent at the D3 receptor among our newly synthesized aporlogues with Ki values of 2.67 and 1.14 nM, respectively. Further assay at the 5-HT1A receptor revealed that aporlogues 7f and 11c also showed high affinity at this receptor with Ki values of 9.68 and 7.59 nM, respectively. They were 3.6- and 6.6-fold more potent at the D3 over 5-HT1A receptors. Such D3/5-HT1A dual property of these compounds may be useful in the treatment of several brain disorders.

Original languageEnglish (US)
Pages (from-to)1999-2008
Number of pages10
JournalBioorganic and Medicinal Chemistry
Issue number6
StatePublished - Mar 15 2011
Externally publishedYes



  • 5-HT receptor
  • Aporphine analogues
  • Arylpiperazine
  • Click reaction
  • Dopamine D receptor

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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