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Endogenous Dopamine Competes with the Binding of a Radiolabeled D3 Receptor Partial Agonist In Vivo: A Positron Emission Tomography Study
Journal article   Peer reviewed

Endogenous Dopamine 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 and Mark A Mintun
Synapse (New York, N.Y.), Vol.65(8), pp.724-732
08/2011
DOI: 10.1002/syn.20891
PMCID: PMC3107898
PMID: 21132811

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Abstract

A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D 3 -selective partial agonist, [ 18 F] 5 . There was variable uptake in regions of brain known to express a high density of D 3 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 D 3 receptor binding in vivo. These data indicate that there is a high level of competition between [ 18 F] 5 and endogenous dopamine for D 3 receptors in vivo.
D3 receptors endogenous dopamine Positron Emission Tomography

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