Development of radioligands for in vivo imaging of GABA(A)-benzodiazepine receptors

Mini Rev Med Chem. 2004 Oct;4(8):909-21. doi: 10.2174/1389557043403332.

Abstract

Changes in the biochemical integrity and function of the GABA(A)-benzodiazepine receptor (BZR) complex have been implicated in various neurological and psychiatric disorders. The development of specific radioligands for the GABA(A)-BZR have not only contributed to the elucidation of the receptor's biochemical functions, but also provided a means by which these changes are correlated to disease states when studied with the functional imaging modalities of positron emission tomography (PET) and single photon emission computed tomography (SPECT).

Publication types

  • Review

MeSH terms

  • Animals
  • Benzodiazepines / metabolism*
  • Benzodiazepines / pharmacokinetics
  • Central Nervous System Diseases / diagnosis
  • Drug Stability
  • Humans
  • Isotope Labeling
  • Ligands
  • Molecular Structure
  • Radioisotopes*
  • Receptors, GABA-A / drug effects
  • Receptors, GABA-A / metabolism*
  • Tomography, Emission-Computed / methods
  • Tomography, Emission-Computed, Single-Photon / methods

Substances

  • Ligands
  • Radioisotopes
  • Receptors, GABA-A
  • Benzodiazepines