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- Title
Analysis of (R)- and (S)-[(11)C]rolipram kinetics in canine myocardium for the evaluation of phosphodiesterase-4 with PET.
- Authors
Lortie M; DaSilva JN; Kenk M; Thorn S; Davis D; Birnie D; Beanlands RS; deKemp RA; Lortie, Mireille; DaSilva, Jean N; Kenk, Miran; Thorn, Stephanie; Davis, Darryl; Birnie, David; Beanlands, Rob S B; deKemp, Robert A
- Abstract
<bold>Purpose: </bold>(R)-[(11)C]rolipram and (S)-[(11)C]rolipram have been proposed to investigate phosphodiesterase-4 and, indirectly, cAMP-mediated signaling with PET. This study assessed binding of these tracers to phosphodiesterase-4 in canine myocardium.<bold>Procedures: </bold>Seven dogs underwent (R)-[(11)C]rolipram and (S)-[(11)C]rolipram dynamic PET imaging at baseline and with co-injection of saturating doses of (R)-rolipram. Dual-input compartment models were applied to estimate the volumes of distribution (V(T)).<bold>Results: </bold>The model comprising one compartment for unmetabolized tracer and one compartment for labeled metabolites provided excellent fits to data acquired with (S)-[(11)C]rolipram at baseline and with both enantiomers during co-injection scans. Use of two compartments for unmetabolized (R)-[(11)C]rolipram at baseline was warranted according to Akaike and Schwarz criteria. V(T) estimates obtained with these models were robust (CV ≤ 8.2%) and reproducible (CV ≤ 15%).<bold>Conclusion: </bold>An important fraction (~65%) of the V (T) of (R)-[(11)C]rolipram at baseline reflects specific binding. Thus, the latter may be a useful index of phosphodiesterase-4 levels in canine myocardium.
- Publication
Molecular Imaging & Biology, 2012, Vol 14, Issue 2, p225
- ISSN
1536-1632
- Publication type
journal article
- DOI
10.1007/s11307-011-0482-6