Aminomethyl-2,6-difluorophenols as a novel class of increased lipophilicity GABA(C) receptor antagonists

Mary Chebib, Graham A.R. Johnston*, Jan P. Mattsson, Karin Rydström, Karolina Nilsson, Jian Qiu, Scott H. Stevenson, Richard B. Silverman

*Corresponding author for this work

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

3- and 4-(Aminomethyl)-2,6-difluorophenols were tested for activity against the three major classes of GABA receptors. 4-(Aminomethyl)-2,6-difluorophenol was shown to be a competitive and somewhat selective antagonist at p1 GABA(C) receptors expressed in Xenopus oocytes (K(B) = 75.5 μM with a 95% Confidence Interval range of 75.2 μM to 75.8 μM). This is the first in a novel class of increased lipophilicity GABA(C) receptor antagonists with little activity at α1β2γ2 GABA(A) and GABA(B) receptors.

Original languageEnglish (US)
Pages (from-to)3093-3098
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume9
Issue number21
DOIs
StatePublished - Nov 1 1999

ASJC Scopus subject areas

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

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