Effect of amperozide on rat cortical 5-HT2 and striatal and limbic dopamine D2 receptor occupancy: Implications for antipsychotic action

Herbert Y. Meltzer*, Zhang Ying Zhang, Craig A. Stockmeier

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

Amperozide (FG 5606, N-ethyl-4-[4′,4′-bis(p-fluorophenyl)butyl]-1-piperazine-carboxamide) is an atypical antipsychotic drug which has relatively weak in vitro affinity for striatal dopamine2 (D2) receptors and strong affinity for cortical 5-HT2 receptors. The in vivo affinity for 5-HT2 binding sites in rat cortex was 1.1 mg/kg. In striatum or olfactory tubercle, doses of amperozide up to 40 mg/kg did not displace radioligand binding to D2 receptors. Amperozide, haloperidol and ritanserin had similar in vivo potency in blocking the 5-HT2 binding site, but only haloperidol displaced D2 receptor binding. Based on the clinically effective dose of amperozide (0.14-0.28 mg/kg per day), it is suggested that the antipsychotic effect of amperozide is related, in part, to its in vivo interaction with the 5-HT2 receptor and that amperozide cannot be expected to exert its antipsychotic action by blockade of D2 receptors in the striatum or limbic regions.

Original languageEnglish (US)
Pages (from-to)67-71
Number of pages5
JournalEuropean Journal of Pharmacology
Volume216
Issue number1
DOIs
StatePublished - May 27 1992

Keywords

  • 5-HT receptors
  • Amperozide
  • Dopamine D receptors

ASJC Scopus subject areas

  • Pharmacology

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