A novel specific binding site for anxiolytic homophthalazines in the rat brain

Cecilia Salamon, Edit J. Horváth, Márton I.K. Fekete, Péter Arányi

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Radioligand binding studies were performed in order to elucidate the mechanism of action of anxiolytic-neuroleptic homophthalazines. Rat striatal membrane preparations were found to bind 3H-EGIS 6775 [3H-GYKI-52 322, 3H-(I-(4-aminophenyl)-4-methyl-7,8-dimethoxy-5H-homophthalazine)] in a specific and displaceable manner. Several other brain regions tested were devoid of similar binding activity. Saturation analysis revealed that binding affinity was in the 10-5-10-7 M range. Binding was enhanced by Mg2+ ions and, to a smaller extent by Ca2+ ions. The binding principle was sensitive to heat or trypsin treatment. This specific binding site appears, according to competition studies, different from the receptors whose presence in the rat striatum has been reported earlier.

Original languageEnglish
Pages (from-to)215-217
Number of pages3
JournalFEBS letters
Volume308
Issue number2
DOIs
Publication statusPublished - Aug 17 1992

Keywords

  • (Rat striatum)
  • Anxiolytic drug. Atypical neuroleptic drug
  • Specific homophthalazine binding

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

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