PET radioligands targeting the brain GABAA /benzodiazepine receptor complex

J Labelled Comp Radiopharm. 2013 Mar-Apr;56(3-4):196-206. doi: 10.1002/jlcr.3008.

Abstract

The development of positron emission tomography radioligands for the GABAA /benzodiazepine receptor complex (GABAA receptor) labeled with (11) C and (18) F is examined. The review covers labeling strategies as well as brief biological evaluations of radioligands. In addition, we assess the special considerations that must be taken during a development program for radioligands targeting the GABAA receptor and explore some of the challenges that lie ahead.

Keywords: F-18; GABA; benzodiazepine; radiochemistry; radioligand.

Publication types

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

MeSH terms

  • Animals
  • Brain / diagnostic imaging*
  • Carbon Radioisotopes / chemistry
  • Fluorine Radioisotopes / chemistry
  • GABA-A Receptor Agonists / chemical synthesis*
  • GABA-A Receptor Agonists / pharmacology
  • GABA-A Receptor Antagonists / chemical synthesis*
  • GABA-A Receptor Antagonists / pharmacology
  • Humans
  • Isotope Labeling*
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacology
  • Receptors, GABA-A / metabolism*

Substances

  • Carbon Radioisotopes
  • Fluorine Radioisotopes
  • GABA-A Receptor Agonists
  • GABA-A Receptor Antagonists
  • Radiopharmaceuticals
  • Receptors, GABA-A