Endogenous dopamine (DA) competes with the binding of a radiolabeled D3 receptor partial agonist in vivo: A positron emission tomography study

Robert H. Mach, Zhude Tu, Jinbin Xu, Shihong Li, Lynne A. Jones, Michelle Taylor, Robert R. Luedtke, Colin P. Derdeyn, Joel S. Perlmutter, Mark A. Mintun

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30 Scopus citations

Abstract

A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D3-selective partial agonist, [18F]5. There was variable uptake in regions of brain known to express a high density of D3 receptors under baseline conditions. Pretreatment with lorazepam (1 mg/kg, i.v. 30 min) to reduce endogenous dopamine activity before tracer injection resulted in a dramatic increase in uptake in the caudate, putamen, and thalamus, and an increase in the binding potential (BP) values, a measure of D3 receptor binding in vivo. These data indicate that there is a high level of competition between [18F]5 and endogenous dopamine for D3 receptors in vivo.

Original languageEnglish
Pages (from-to)724-732
Number of pages9
JournalSynapse
Volume65
Issue number8
DOIs
StatePublished - Aug 2011

Keywords

  • D receptors
  • Endogenous DA
  • Positron emission tomography

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    Mach, R. H., Tu, Z., Xu, J., Li, S., Jones, L. A., Taylor, M., Luedtke, R. R., Derdeyn, C. P., Perlmutter, J. S., & Mintun, M. A. (2011). Endogenous dopamine (DA) competes with the binding of a radiolabeled D3 receptor partial agonist in vivo: A positron emission tomography study. Synapse, 65(8), 724-732. https://doi.org/10.1002/syn.20891