Ethers of 3-hydroxyphenylacetic acid as selective gamma-hydroxybutyric acid receptor ligands

Weibin Chen, Huifang Wu, R. Jason Hernandez, Ashok K. Mehta, Maharaj K. Ticku, Charles P. France, Andrew Coop

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Gamma-hydroxybutyric acid (GHB) is a drug of abuse, a therapeutic, and purportedly a neurotransmitter with a complex mechanism of action in vivo due to direct actions at GABAB as well as GHB receptors and because of its metabolism to GABA. Herein, we describe 3-ethers of 3-hydroxyphenylacetic acid, which have relatively high affinity at GHB sites, no significant affinity at GABA receptors, and would not be expected to be rapidly metabolized to GABAergic ligands. The selectivity of these compounds (UMB108, UMB109, and UMB119) could prove to be useful for studying the biology of GHB receptors, free from GABAergic effects.

Original languageEnglish (US)
Pages (from-to)3201-3202
Number of pages2
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number13
DOIs
StatePublished - Jul 1 2005

Keywords

  • Drug abuse
  • GABA
  • GHB

ASJC Scopus subject areas

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

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