In vivo stereospecific [3H]spiperone binding in rat brain: Characteristics, regional distribution, kinetics and pharmacological properties

Domenico Barone, Franco Luzzani, Alessandro Assandri, Giulio Galliani, Tiziana Mennini, Silvio Garattini

Research output: Contribution to journalArticle

Abstract

The time course of [3H]spiperone distribution in the three major pools (specifically and non-specifically membrane-bound and soluble) of different brain areas, was studied in rats given a tracer amount of the drug. In addition, the stereospecificity, dissociation kinetics and pharmacological nature of the in vivo bound [3H]spiperone were investigated. The data show that [3H]spiperone binding sites in the striatum, olfactory tubercles and hypophysis differ clearly from those of the cortical regions. In the prevalently dopaminergic areas the amount of ligand bound to membranes is, up to 24 h post-treatment, proportional to the total 3H present. However a more correct analysis of the data was obtained in all the experiments when membrane-bound was measured instead of total radioactivity. Thus assay of the in vivo specifically bound [3H]spiperone appears essential for a correct evaluation of the density, affinity, regional distribution, pharmacological nature and kinetics of the drug-receptor interaction.

Original languageEnglish
Pages (from-to)63-74
Number of pages12
JournalEuropean Journal of Pharmacology
Volume116
Issue number1-2
DOIs
Publication statusPublished - Oct 8 1985

Keywords

  • Brain receptors
  • [H]Spiperone binding

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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