| Kinetic analysis of technetium-99m-labeled nitroimidazole (BMS-181321) as a tracer of myocardial hypoxia. | |
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MedLine Citation:
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PMID: 7648674 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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BACKGROUND: Experimental data have indicated that [99mTc]-nitroimidazole (BMS-181321) is preferentially taken up in hypoxic tissue; its kinetics, however, has not been fully investigated. The purpose of this study was to address the relation between perfusate oxygen level and myocardial retention of [99mTc]nitroimidazole. METHODS AND RESULTS: Bolus injection and constant infusion experiments were performed in Langendorff buffer-perfused rat hearts in normoxic and hypoxic conditions. Data were acquired with a pair of NaI detectors. The initial clearance rate of [99mTc]nitroimidazole was approximately 20 seconds and independent of perfusate oxygen level. The slow clearance rate was greater than 3 hours in all perfusion conditions. The tissue retention of [99mTc]nitroimidazole varied from 0.61 +/- 0.14% in normoxic conditions to 5.94 +/- 1.16% in the most severe hypoxic conditions. In addition, tissue retention was inversely proportional to perfusate oxygen level in a sigmoidal manner. The constant infusion experiments established that the binding rate at 25% oxygen level (1.94 +/- 0.38 mL of perfusate/min-g dry wt) was twofold of that at 40% and sevenfold at 100%. The binding rate of [99mTc]nitroimidazole was independent of the perfusion sequence, suggesting irreversible binding. CONCLUSIONS: These data indicate that [99mTc]nitroimidazole may be a useful tracer for the identification of myocardial hypoxia. A sigmoidal relation was demonstrated for the uptake of the tracer, which suggests that a threshold level of hypoxia is necessary for the uptake of the tracer. |
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Authors:
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C K Ng; A J Sinusas; B L Zaret; R Soufer |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Circulation Volume: 92 ISSN: 0009-7322 ISO Abbreviation: Circulation Publication Date: 1995 Sep |
Date Detail:
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Created Date: 1995-09-25 Completed Date: 1995-09-25 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0147763 Medline TA: Circulation Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1261-8 Citation Subset: AIM; IM |
Affiliation:
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Yale University-VA Positron Emission Tomography Center, West Haven, CT 06516, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cell Hypoxia Heart / radionuclide imaging* Male Myocardial Ischemia / metabolism, radionuclide imaging* Myocardium / metabolism Nitroimidazoles / diagnostic use*, pharmacokinetics Organotechnetium Compounds / diagnostic use*, pharmacokinetics Oxygen Consumption / physiology Perfusion Rats Rats, Sprague-Dawley Sodium Pertechnetate Tc 99m / diagnostic use, pharmacokinetics Technetium Tc 99m Pentetate / diagnostic use, pharmacokinetics Time Factors |
| Chemical | |
Reg. No./Substance:
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0/Nitroimidazoles; 0/Organotechnetium Compounds; 149447-21-2/BMS 181321; 23288-60-0/Sodium Pertechnetate Tc 99m; 65454-61-7/Technetium Tc 99m Pentetate |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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