Vandehey, Nicholas T;
Moirano, Jeffrey M;
Converse, Alexander K;
Holden, James E;
Mukherjee, Jogesh;
Murali, Dhanabalan;
Nickles, R Jerry;
Davidson, Richard J;
Schneider, Mary L;
Christian, Bradley T
High-Affinity Dopamine D2/D3 PET Radioligands 18F-Fallypride and 11C-FLB457: A Comparison of Kinetics in Extrastriatal Regions Using a Multiple-Injection Protocol
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Medientyp:
E-Artikel
Titel:
High-Affinity Dopamine D2/D3 PET Radioligands 18F-Fallypride and 11C-FLB457: A Comparison of Kinetics in Extrastriatal Regions Using a Multiple-Injection Protocol
Beteiligte:
Vandehey, Nicholas T;
Moirano, Jeffrey M;
Converse, Alexander K;
Holden, James E;
Mukherjee, Jogesh;
Murali, Dhanabalan;
Nickles, R Jerry;
Davidson, Richard J;
Schneider, Mary L;
Christian, Bradley T
Erschienen:
SAGE Publications, 2010
Erschienen in:
Journal of Cerebral Blood Flow & Metabolism, 30 (2010) 5, Seite 994-1007
Sprache:
Englisch
DOI:
10.1038/jcbfm.2009.270
ISSN:
0271-678X;
1559-7016
Entstehung:
Anmerkungen:
Beschreibung:
18F-Fallypride and 11C-FLB457 are commonly used PET radioligands for imaging extrastriatal dopamine D2/D3 receptors, but differences in their in vivo kinetics may affect the sensitivity for measuring subtle changes in receptor binding. Focusing on regions of low binding, a direct comparison of the kinetics of 18F-fallypride and 11C-FLB457 was made using a MI protocol. Injection protocols were designed to estimate K1, k2, fND kon, Bmax, and koff in the midbrain and cortical regions of the rhesus monkey. 11C-FLB457 cleared from the arterial plasma faster and yielded a ND space distribution volume ( K1/ k2) that is three times higher than 18F-fallypride, primarily due to a slower k2 (FAL:FLB; k2=0.54 min−1:0.18 min−1). The dissociation rate constant, koff, was slower for 11C-FLB457, resulting in a lower KDapp than 18F-fallypride (FAL:FLB; 0.39 nM:0.13 nM). Specific D2/D3 binding could be detected in the cerebellum for 11C-FLB457 but not 18F-fallypride. Both radioligands can be used to image extrastriatal D2/D3 receptors, with 11C-FLB457 providing greater sensitivity to subtle changes in low-receptor-density cortical regions and 18F-fallypride being more sensitive to endogenous dopamine displacement in medium-to-high-receptor-density regions. In the presence of specific D2/D3 binding in the cerebellum, reference region analysis methods will give a greater bias in BPND with 11C-FLB457 than with 18F-fallypride.