Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists

Kirsten T. Tolentino, Viktoriya Mashinson, Anish K. Vadukoot, Corey R. Hopkins

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


The dopamine receptor 4 (D4R) is highly expressed in both motor, associative and limbic subdivisions of the cortico-basal ganglia network. Due to the distribution in the brain, there is mounting evidence pointing to a role for the D4R in the modulation of this network and its subsequent involvement in L-DOPA induced dyskinesias in Parkinson's disease. As part of our continued effort in the discovery of novel D4R antagonists, we report the discovery and characterization of a new 3- or 4-benzyloxypiperidine scaffold as D4R antagonists. We report several D4R selective compounds (>30-fold vs. other dopamine receptor subtypes) with improved in vitro and in vivo stability over previously reported D4R antagonists.

Original languageEnglish (US)
Article number128615
JournalBioorganic and Medicinal Chemistry Letters
StatePublished - Apr 1 2022


  • Antagonists
  • Benzyloxypiperidine
  • D4R
  • Dopamine 4 receptor
  • Parkinson's disease

ASJC Scopus subject areas

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


Dive into the research topics of 'Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists'. Together they form a unique fingerprint.

Cite this