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Wiley, Synapse, 8(65), p. 724-732, 2011

DOI: 10.1002/syn.20891

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

Journal article published in 2011 by Robert H. Mach, Zhude Tu ORCID, Jinbin Xu, Shihong Li, Lynne A. Jones, Michelle Taylor, Robert R. Luedtke, Colin P. Derdeyn ORCID, Joel S. Perlmutter, Mark A. Mintun
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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 prior to 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.