3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT2B, 5-HT7, or σ1 Receptor Ligands

Matthew R. Porter, Haiyan Xiao, Jing Wang, Sylvia B. Smith, Joseph J. Topczewski

Research output: Contribution to journalArticle

Abstract

The phenethylamine backbone is a privileged substructure found in a wide variety of G protein-coupled receptor (GPCR) ligands. This includes both endogenous neurotransmitters and active pharmaceutical agents. More than 20 structurally unique heterocyclic phenethylamine derivatives were broadly evaluated for GPCR affinity. Selective ligands for the 5-HT2B, 5-HT7, and σ1 receptors were identified, each with low nanomolar binding affinities. The σ1 receptor affinity was supported in a cellular assay that provided evidence for increased cell survival under oxidative stress.

Original languageEnglish (US)
Pages (from-to)1436-1442
Number of pages7
JournalACS Medicinal Chemistry Letters
Volume10
Issue number10
DOIs
StatePublished - Oct 10 2019

Keywords

  • 5-HT
  • G protein-coupled receptors
  • neuroprotection
  • serotonin receptors
  • σ receptor
  • σ receptor

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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