Measuring drug occupancy in the absence of a reference region: the Lassen plot re-visited

Vincent J. Cunningham, Eugenii A. Rabiner, Mark Slifstein, Marc Laruelle, Roger N. Gunn

Research output: Contribution to journalArticle

154 Citations (Scopus)

Abstract

Quantitative estimation of neuroreceptor occupancy by exogenous drugs using positron emission tomography is based on the reduction in the total volume of distribution (VT) of site-specific radioligands after drug administration. An estimate of the distribution volume of free and nonspecifically bound radioligand (VND) is also required to distinguish specific from total binding. However, a true reference region, devoid of specific binding, is often not available. We present a transformation of a graphical method, originally introduced by Lassen, using regional estimates of VT alone to determine occupancy, together with an extension that does not require baseline data.

Original languageEnglish
Pages (from-to)46-50
Number of pages5
JournalJournal of Cerebral Blood Flow and Metabolism
Volume30
Issue number1
Early online date9 Sep 2009
DOIs
Publication statusPublished - Jan 2010

Keywords

  • graphical analysis
  • occupancy
  • PET
  • positron-emission-tomography
  • brain transfer constants
  • time uptake data
  • in-vivo
  • binding
  • receptors
  • humans
  • model

Cite this