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

J Neural Transm (Vienna). 2007 Sep;114(9):1143-6. doi: 10.1007/s00702-007-0784-7. Epub 2007 Jul 6.


The effect of (-)-OSU6162 on the incorporation of GTPgammaS(35) in the membranes of hD(2l)-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 100 nM) 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.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Dopamine / physiology*
  • Dopamine D2 Receptor Antagonists*
  • Dose-Response Relationship, Drug
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Piperidines / pharmacology*
  • Receptors, Dopamine D2 / agonists*
  • Receptors, Dopamine D2 / physiology


  • Dopamine D2 Receptor Antagonists
  • Piperidines
  • Receptors, Dopamine D2
  • OSU 6162
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Dopamine