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Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET

We have developed a feedback-controlled bolus plus infusion (FC-B/I) method for monitoring the interaction between positron emission tomography (PET) ligands and their specific target molecules with PET. The usefulness of the FC-B/I method was evaluated by the direct interaction between [(11)C]raclo...

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Autores principales: Ohba, Hiroyuki, Harada, Norihiro, Nishiyama, Shingo, Kakiuchi, Takeharu, Kimura, Yuichi, Tsukada, Hideo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3597362/
https://www.ncbi.nlm.nih.gov/pubmed/22968323
http://dx.doi.org/10.1038/jcbfm.2012.134
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author Ohba, Hiroyuki
Harada, Norihiro
Nishiyama, Shingo
Kakiuchi, Takeharu
Kimura, Yuichi
Tsukada, Hideo
author_facet Ohba, Hiroyuki
Harada, Norihiro
Nishiyama, Shingo
Kakiuchi, Takeharu
Kimura, Yuichi
Tsukada, Hideo
author_sort Ohba, Hiroyuki
collection PubMed
description We have developed a feedback-controlled bolus plus infusion (FC-B/I) method for monitoring the interaction between positron emission tomography (PET) ligands and their specific target molecules with PET. The usefulness of the FC-B/I method was evaluated by the direct interaction between [(11)C]raclopride, a dopamine D(2) receptor (D(2)R) ligand, and cold raclopride (10 and 100 μg/kg) in the brains of conscious monkeys. The present results demonstrated that the FC-B/I method could achieve the equilibrium state of [(11)C]raclopride in the striatum of monkey brain, and also that the cold raclopride-induced reduction of [(11)C]raclopride binding to D(2)R was observed in a dose-dependent manner. Good correlations of distribution volume ratio of the striatum to cerebellum between the conventional bolus plus infusion (B/I) method and the FC-B/I method as well as between the conventional bolus injection method and the FC-B/I method were observed. These results indicated that the system could be a useful tool for the evaluation of interaction between drug candidates and their target molecules like enzymes, receptors, and transporters by using of their specific PET ligands.
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spelling pubmed-35973622013-03-15 Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET Ohba, Hiroyuki Harada, Norihiro Nishiyama, Shingo Kakiuchi, Takeharu Kimura, Yuichi Tsukada, Hideo J Cereb Blood Flow Metab Original Article We have developed a feedback-controlled bolus plus infusion (FC-B/I) method for monitoring the interaction between positron emission tomography (PET) ligands and their specific target molecules with PET. The usefulness of the FC-B/I method was evaluated by the direct interaction between [(11)C]raclopride, a dopamine D(2) receptor (D(2)R) ligand, and cold raclopride (10 and 100 μg/kg) in the brains of conscious monkeys. The present results demonstrated that the FC-B/I method could achieve the equilibrium state of [(11)C]raclopride in the striatum of monkey brain, and also that the cold raclopride-induced reduction of [(11)C]raclopride binding to D(2)R was observed in a dose-dependent manner. Good correlations of distribution volume ratio of the striatum to cerebellum between the conventional bolus plus infusion (B/I) method and the FC-B/I method as well as between the conventional bolus injection method and the FC-B/I method were observed. These results indicated that the system could be a useful tool for the evaluation of interaction between drug candidates and their target molecules like enzymes, receptors, and transporters by using of their specific PET ligands. Nature Publishing Group 2013-01 2012-09-12 /pmc/articles/PMC3597362/ /pubmed/22968323 http://dx.doi.org/10.1038/jcbfm.2012.134 Text en Copyright © 2013 International Society for Cerebral Blood Flow & Metabolism, Inc. http://creativecommons.org/licenses/by-nc-nd/3.0/ This work is licensed under the Creative Commons Attribution-NonCommercial-No Derivative Works 3.0 Unported License. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-nd/3.0/
spellingShingle Original Article
Ohba, Hiroyuki
Harada, Norihiro
Nishiyama, Shingo
Kakiuchi, Takeharu
Kimura, Yuichi
Tsukada, Hideo
Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title_full Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title_fullStr Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title_full_unstemmed Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title_short Feedback-controlled bolus plus infusion (FC-B/I) method for quantitative drug assessment in living brain with PET
title_sort feedback-controlled bolus plus infusion (fc-b/i) method for quantitative drug assessment in living brain with pet
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3597362/
https://www.ncbi.nlm.nih.gov/pubmed/22968323
http://dx.doi.org/10.1038/jcbfm.2012.134
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