Radioligands for the dopamine receptor subtypes

J Labelled Comp Radiopharm. 2013 Mar-Apr;56(3-4):130-48. doi: 10.1002/jlcr.3000.

Abstract

The actions of the predominant neurotransmitter in the brain, dopamine, are mediated by the postsynaptic dopamine receptors. The five dopamine receptor subtypes and their regulation have been associated with a large variety of psychiatric diseases. Therefore, positron emission tomography (PET) imaging studies using suitable and selective (18) F-labeled and (11) C-labeled dopamine receptor radioligands could provide valuable knowledge on the impact of receptor density on the pathogenesis and evolvement of neuropsychiatric and neurological diseases. This special issue subchapter provides a summary of the most important (18) F-labeled and (11) C-labeled radioligands for PET imaging of the dopamine receptor subtypes, their radiochemistry, and characteristics from in vitro and in vivo applications, considering not only the already established PET ligands but also the recently published preclinical work.

Keywords: 11C; 18F; PET; dopamine receptor; positron emission tomography; radioligand.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Carbon Radioisotopes / chemistry
  • Dopamine Agonists / chemical synthesis
  • Dopamine Agonists / pharmacology*
  • Dopamine Antagonists / chemical synthesis
  • Dopamine Antagonists / pharmacology*
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Positron-Emission Tomography
  • Protein Binding
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacology*
  • Receptors, Dopamine / metabolism*
  • Substrate Specificity

Substances

  • Carbon Radioisotopes
  • Dopamine Agonists
  • Dopamine Antagonists
  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Dopamine