Abstract:
:The present study was undertaken to investigate if pretreatment with pharmacological agents could change the organ uptake of 11C-labelled L-DOPA, and especially if the urinary excretion could be decreased. L-[beta-11C]DOPA was injected IV into unanesthetized Sprague-Dawley rats. After 20 min the rats were decapitated and organs taken out for radioactivity measurements. The uptake in the organs was investigated in animals only given the tracer, and in animals pretreated with drugs such as decarboxylase inhibitors carbidopa and benserazide as well as the monoamine oxidase inhibitors deprenyl, clorgyline, and the COMT inhibitor OR-486. A marked decrease in the urinary radioactivity was observed after carbidopa and benserazide administration. HPLC analysis revealed that under native conditions the major part of urinary radioactivity existed as dopamine, which was eliminated by the decarboxylase inhibitors. After pretreatment with the COMT inhibitor OR-486, the radioactivity uptake in the pancreas increased fourfold as compared to non-treated animals. HPLC analysis showed that this correlated with a marked increase in radiolabelled DOPAC. In the other organs and with the other drugs, only small effects were observed. With L-[beta-11C]fluoroDOPA as a tracer, similar results were observed although the increase in the pancreas by OR-486 had a lower magnitude. These studies suggest that it might be possible to improve the diagnostic ratio of L-[beta-11C]DOPA or L-[18F]fluoroDOPA in whole-body PET studies by pretreating the patient with decarboxylase inhibitor for reducing the urinary excretion and potentially increase the target organ uptake by COMT inhibition.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Bergström M,Lu L,Marquez M,Fasth KJ,Bjurling P,Watanabe Y,Eriksson B,Långström Bdoi
10.1016/s0969-8051(96)00149-7subject
Has Abstractpub_date
1997-01-01 00:00:00pages
15-9issue
1eissn
0969-8051issn
1872-9614pii
S0969805196001497journal_volume
24pub_type
杂志文章abstract::Indium-111 labeled, Trastuzumab-Doxorubicin Conjugated, and APTES-PEG coated magnetic nanoparticles were designed for tumor targeting, drug delivery, controlled drug release, and dual-modal tumor imaging. Superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by thermal decomposition method to obtain nar...
journal_title:Nuclear medicine and biology
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journal_title:Nuclear medicine and biology
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pub_type: 杂志文章,评审
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更新日期:2002-01-01 00:00:00
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更新日期:1999-08-01 00:00:00
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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更新日期:1994-02-01 00:00:00
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journal_title:Nuclear medicine and biology
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更新日期:1995-02-01 00:00:00
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pub_type: 杂志文章
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更新日期:1996-02-01 00:00:00
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pub_type: 杂志文章
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更新日期:2013-02-01 00:00:00
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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更新日期:2005-10-01 00:00:00
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pub_type: 杂志文章
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更新日期:2016-06-01 00:00:00
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journal_title:Nuclear medicine and biology
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更新日期:2012-10-01 00:00:00
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pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2011.01.007
更新日期:2011-07-01 00:00:00