PET radioligands for the vesicular transporters for monoamines and acetylcholine

J Labelled Comp Radiopharm. 2013 Mar-Apr;56(3-4):167-71. doi: 10.1002/jlcr.2998.

Abstract

The vesicular transporters for the monoamine and acetylcholine have been successfully targeted for the development of radioligands for human brain imaging. The vesicular monoamine transporter type 2 ligands are based on the structure of tetrabenazine, a known clinically used drug. In contrast, the radioligands for vesicular acetylcholine transporter are based on vesamicol, a toxic xenobiotic. The similarities and differences in the development of these two classes of radioligands are discussed.

Keywords: brain; carbon-11; fluorine-18; transporter; vesicular.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Carbon Radioisotopes / chemistry
  • Fluorine Radioisotopes / chemistry
  • Humans
  • Ligands
  • Positron-Emission Tomography*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / pharmacology*
  • Vesicular Acetylcholine Transport Proteins / metabolism*
  • Vesicular Monoamine Transport Proteins / metabolism*

Substances

  • Carbon Radioisotopes
  • Fluorine Radioisotopes
  • Ligands
  • Radiopharmaceuticals
  • Vesicular Acetylcholine Transport Proteins
  • Vesicular Monoamine Transport Proteins