Profile of in Vitro Binding Affinities of Neuroleptics at Different Rat Brain Receptors: Cluster Analysis Comparison with Pharmacological and Clinical Profiles

Rodolfo Testa, Gianalfredo Abbiati, Roberto Ceserani, Gianvico Restelli, Alessandro Vanasia, Domenico Barone, Marco Gobbi, Tiziana Mennini

Research output: Contribution to journalArticlepeer-review

Abstract

A series of 21 neuroleptics with different chemical structures (phenothiazines, thioxanthenes, dibenzodiazepines, butyrophenones, benzamides, etc.) was examined for their in vitro interactions with 12 neurotransmitter binding sites in the rat brain (alpha- and beta-noradrenergic, dopaminergic, muscarinic, serotoninergic, histaminic, and opioid receptors, calcium channels, and serotonin uptake binding sites). The biochemical profile obtained from the binding data was compared with reported pharmacological and clinical profiles for this class of compounds by cluster analysis. Cluster analysis on binding data classified the compounds in three main subgroups: benzamides, compounds with an affinity mainly for DA2 and 5-HT2 receptors and inactive at muscarinic receptors, and compounds with a high affinity for alpha 1-adrenergic receptors and muscarinic receptors. The main subgroups resulting from cluster analysis of previously published pharmacological and clinical data for neuroleptics contain compounds common to the present study, with some correlations. The results extend previous observations that a complete binding profile corresponds to the pharmacological and clinical profile of this class of compounds.

Original languageEnglish
Pages (from-to)571-577
Number of pages7
JournalPharmaceutical Research
Volume6
Issue number7
DOIs
Publication statusPublished - 1989

Keywords

  • cluster analysis
  • neuroleptics
  • profiles
  • receptor binding assays

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Organic Chemistry
  • Pharmacology (medical)
  • Pharmaceutical Science
  • Pharmacology
  • Chemistry(all)

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