Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist

Jinbin Xu, Suwanna Vangveravong, Shihong Li, Jinda Fan, Lynne A. Jones, Jinquan Cui, Ruike Wang, Zhude Tu, Wenhua Chu, Joel S. Perlmutter, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

A series of microPET imaging studies were conducted in anesthetized rhesus monkeys using the dopamine D2-selective partial agonist, [11C]SV-III-130. There was a high uptake in regions of brain known to express a high density of D2 receptors under baseline conditions. Rapid displacement in the caudate and putamen, but not in the cerebellum, was observed after injection of the dopamine D2/3 receptor nonselective ligand S(-)-eticlopride at a low dosage (0.025mg/kg/i.v.); no obvious displacement in the caudate, putamen and cerebellum was observed after the treatment with a dopamine D3 receptor selective ligand WC-34 (0.1mg/kg/i.v.). Pretreatment with lorazepam (1mg/kg, i.v. 30min) to reduce endogenous dopamine prior to tracer injection resulted in unchanged binding potential (BP) values, a measure of D2 receptor binding in vivo, in the caudate and putamen. d-Amphetamine challenge studies indicate that there is a significant displacement of [11C]SV-III-130 by d-Amphetamine-induced increases in synaptic dopamine levels.

Original languageEnglish
Pages (from-to)168-174
Number of pages7
JournalNeuroImage
Volume71
DOIs
StatePublished - May 1 2013

Keywords

  • Dopamine
  • Dopamine D receptors
  • Positron emission tomography

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