D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs

B. L. Roth*, S. Tandra, L. H. Burgess, D. R. Sibley, H. Y. Meltzer

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

138 Scopus citations

Abstract

The affinities of 13 atypical and 12 typical antipsychotic drugs for the cloned rat D4 dopamine receptor and the D4/D2 ratios were examined. Of the atypical antipsychotic drugs tested, only clozapine, risperidone, olanzapine, zotepine and tiospirone had affinities less than 20 nM. In fact, many atypical antipsychotic drugs had relatively low affinities for the cloned rat D4 receptor, with Ki values greater than 100 nM (Seroquel, fluperlapine, tenilapine, FG5803 and melperone). Additionally, several typical antipsychotic drugs had high affinities for the cloned rat D4 receptor, with Kis less than 20 nM (loxapine, chlorpromazine, fluphenazine, mesoridazine, thioridazine and trifluoroperazine). The ratios of D2/D4 affinities did not differentiate between these two types of antipsychotic drugs. Thus, D4 dopamine receptor affinity, used as a single measure, does not distinguish between the group of typical and atypical antipsychotic drugs analyzed.

Original languageEnglish (US)
Pages (from-to)365-368
Number of pages4
JournalPsychopharmacology
Volume120
Issue number3
DOIs
StatePublished - Aug 1995

Keywords

  • Antipsychotic drugs
  • D dopamine receptor
  • Rat

ASJC Scopus subject areas

  • Pharmacology

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