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J Cereb Blood Flow Metab. 2010 Jan;30(1):46-50. doi: 10.1038/jcbfm.2009.190. Epub 2009 Sep 9.

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

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1
GlaxoSmithKline, Clinical Imaging Centre, Hammersmith Hospital, London, UK. vincent.j.cunningham@gsk.com

Abstract

Quantitative estimation of neuroreceptor occupancy by exogenous drugs using positron emission tomography is based on the reduction in the total volume of distribution (V(T)) of site-specific radioligands after drug administration. An estimate of the distribution volume of free and nonspecifically bound radioligand (V(ND)) 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 V(T) alone to determine occupancy, together with an extension that does not require baseline data.

PMID:
19738632
PMCID:
PMC2949110
DOI:
10.1038/jcbfm.2009.190
[Indexed for MEDLINE]
Free PMC Article
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