Analysis of (R)- and (S)-[(11)C]rolipram kinetics in canine myocardium for the evaluation of phosphodiesterase-4 with PET.
Purpose: (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.Procedures: Seven dogs underwent (R)-[(11)C]rolipram...
| Publicado en: | Molecular Imaging & Biology Vol. 14; no. 2; pp. 225 - 237 |
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| Autores principales: | , , , , , , , , , , , , , , , |
| Formato: | research Journal Article |
| Publicado: |
Springer Nature
Apr2012
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=104442872&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 104442872 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 15361632 KJU jtl: Molecular Imaging & Biology issn: 15361632 maglogo: N pubinfo: dt: Apr2012 vid: 14 iid: 2 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 104442872 104442872 NLM21424298 2011751383 10.1007/s11307-011-0482-6 NLM21424298 104442872 ppf: 225 ppct: 12 formats: fmt: @attributes: type: P tig: atl: Analysis of (R)- and (S)-[(11)C]rolipram kinetics in canine myocardium for the evaluation of phosphodiesterase-4 with PET. aug: au: 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 affil: Cardiac PET Centre, University of Ottawa Heart Institute, Ottawa, Ontario, Canada, K1Y 4W7 sug: subj: Esterases Metabolism Heterocyclic Compounds Heterocyclic Compounds Pharmacokinetics Myocardium Tomography, Emission-Computed Methods Animal Studies Chemistry Dogs Heterocyclic Compounds Blood Models, Biological Radioisotopes Diagnostic Use Time Factors ab: Purpose: (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.Procedures: 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)).Results: 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%).Conclusion: 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. pubtype: Academic Journal doctype: research Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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