Journal
JOURNAL OF NEURAL TRANSMISSION
Volume 114, Issue 9, Pages 1143-1146Publisher
SPRINGER WIEN
DOI: 10.1007/s00702-007-0784-7
Keywords
partial dopamine agonist; dopamine; GTPgammaS(35); psychosis
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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.
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