Typical antipsychotics exhibit inverse agonist activity at rat dopamine D1-like receptors expressed in Sf9 cells

Michael W. Martin, Allelia W. Scott, Douglas E. Johnston, Suzy Griffin, Robert R. Luedtke

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

The baculovirus system has been used to express the rat dopamine D1 receptors in Spodoptera frugiperda (Sf9) cells. A panel of typical antipsychotics including, α-flupenthixol, fluphenazine and thioridizine were found to inhibit dopamine-dependent stimulation of adenylyl cyclase. However, these compounds were also found to inhibit adenylyl cyclase activity in the absence of agonist in Sf9 cells expressing dopamine D1-like receptors. Therefore, these nonselective dopamine receptor compounds displayed negative intrinsic or inverse agonist activity. None of the compounds tested were neutral antagonists.

Original languageEnglish
Pages (from-to)73-82
Number of pages10
JournalEuropean Journal of Pharmacology
Volume420
Issue number2-3
DOIs
StatePublished - 25 May 2001

Keywords

  • Adenylyl cyclase stimulation
  • Antipsychotic
  • Baculovirus expression
  • Dopamine D1 receptor
  • Dopamine receptor
  • Inverse agonist

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