Transport across the blood-brain barrier: stereoselectivity and PET-tracers.

Abstract:

:This article reviews positron emission tomography (PET) studies of labeled enantiomers of different PET-tracers from the early 1980s. Comparative studies on stereoselective behavior of the transport of tracers across the blood-brain barrier (BBB) are discussed. Tracers are transported through the BBB into the brain, via diffusion or via several transport systems. These transport systems are able to transport endogenous and exogenous compounds from the blood into the brain, and visa versa. A clear difference exists in BBB transport of the enantiomers of several tracers. In addition, in most cases, binding of these labeled enantiomers to receptors/transporters is stereoselective. Finally, use of the biological inactive labeled enantiomer for the measurement of nonspecific binding is discussed. Given the differences in transport and binding, it is concluded that quantitative PET studies can only be performed using pure enantiomers.

journal_name

Mol Imaging Biol

authors

Luurtsema G,de Lange EC,Lammertsma AA,Franssen EJ

doi

10.1016/j.mibio.2004.06.008

keywords:

subject

Has Abstract

pub_date

2004-09-01 00:00:00

pages

306-18

issue

5

eissn

1536-1632

issn

1860-2002

pii

S1536-1632(04)00268-9

journal_volume

6

pub_type

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