Stimulating and inhibitory effects of the dopamine "stabilizer" (-)-OSU6162 on dopamine D2 receptor function in vitro

R. A. Lahti, C. A. Tamminga, A. Carlsson

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

The effect of (-)-OSU6162 on the incorporation of GTPgammaS35 in the membranes of hD2l-transfected CHO cells was investigated. In the absence of dopamine the compound exerted a slight but significant stimulating action, suggesting a weak partial agonism. In the presence of dopamine, low concentrations (10 to 100nM) enhanced the stimulating action of dopamine. This enhancing effect was reversed by higher concentrations of (-)-OSU6162 in a complex biphasic manner. The dopamine-enhancing action is proposed to be mediated by binding to an allosteric site with high affinity and the inhibitory component by a low-affinity binding to the orthosteric site of the dopamine receptor.

Original languageEnglish (US)
Pages (from-to)1143-1146
Number of pages4
JournalJournal of Neural Transmission
Volume114
Issue number9
DOIs
StatePublished - Sep 1 2007

Keywords

  • Dopamine
  • GTPgammaS
  • Partial dopamine agonist
  • Psychosis

ASJC Scopus subject areas

  • Neurology
  • Clinical Neurology
  • Psychiatry and Mental health
  • Biological Psychiatry

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