Parametric images of benzodiazepine receptor concentration using a partial-saturation injection

J Cereb Blood Flow Metab. 1997 Mar;17(3):343-55. doi: 10.1097/00004647-199703000-00011.

Abstract

The in vivo quantification of the benzodiazepine receptor concentration in human brain using positron emission tomography (PET) and 11C-flumazenil (11C-FMZ), is usually based on a three-compartment model and on PET curves measured in a small number of large regions of interest; however, it should be interesting to estimate the receptor concentration for each pixel and to build quantified images of the receptor concentration. The main advantage is to allow screening of the receptor site localization and visual observation of the possible abnormalities. Up to now, all the methods described include complex experimental protocols, difficult to use in routine examinations. In this paper, we propose the partial-saturation approach to obtain parametric images of benzodiazepine receptor concentration and FMZ affinity. It consists of a single FMZ injection with a low specific activity, followed by Scatchard analysis. Like other parametric imaging methods, this partial-saturation approach can lead to a small percentage (< 1%) of unrealistic values in receptor-poor regions; however, it is the only method that allows receptor concentration and affinity images to be obtained from a single-injection 40-min experiment without blood sampling. We also propose a second method in which the receptor concentration map is directly deduced from the PET image acquired 5 to 10 min after a partial-saturation injection. This method assumes a known and constant FMZ affinity value but requires only very simple corrections of this PET image. It is robust (negative values are never found) and quite simple to use in routine examination of patients (no blood sampling, single injection, only 10-min experiment).

MeSH terms

  • Brain Chemistry*
  • Flumazenil* / administration & dosage
  • Flumazenil* / metabolism
  • Flumazenil* / pharmacokinetics
  • GABA Modulators* / administration & dosage
  • GABA Modulators* / metabolism
  • GABA Modulators* / pharmacokinetics
  • Humans
  • Image Processing, Computer-Assisted
  • Models, Biological
  • Nerve Tissue Proteins / analysis*
  • Nerve Tissue Proteins / metabolism
  • Receptors, GABA-A / analysis*
  • Receptors, GABA-A / metabolism
  • Tomography, Emission-Computed*

Substances

  • GABA Modulators
  • Nerve Tissue Proteins
  • Receptors, GABA-A
  • Flumazenil