Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors

Research output: Contribution to journalJournal articleResearchpeer-review

  • Marie Kueny-Stotz
  • Stefan Chassaing
  • Raymond Brouillard
  • Mogens Peter Cherly Nielsen
  • Maurice Goeldner
The synthesis of a series of derivatized flavylium cations was undertaken and the affinity to the benzodiazepine binding site of the GABA-A receptor evaluated. The observed high affinity for some derivatives (sub-muM range) was explained by an in vitro transformation of the flavylium cations into the corresponding trans-retrochalcones, components which are proposed to be the active species in this series.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Issue number17
Pages (from-to)4864-4867
Publication statusPublished - 2008

Bibliographical note

Keywords: Animals; Benzodiazepines; Binding Sites; Brain; Chalcones; Flavonoids; Fluorides; Ligands; Male; Phosphates; Polycyclic Hydrocarbons, Aromatic; Rats; Rats, Wistar; Receptors, GABA-A; Salts

ID: 10161334