Document Detail


99mTc-MAMA-chrysamine G, a probe for beta-amyloid protein of Alzheimer's disease.
MedLine Citation:
PMID:  10552079     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Chrysamine G (CG), an analogue of Congo red, is known to bind in vitro to the beta-amyloid protein (Abeta 10-43) and to homogenates of several regions of the brain of Alzheimer's disease (AD) patients. We synthesised a conjugate of 2-(acetamido)-CG with a bis-S-trityl protected monoamide-monoaminedithiol (MAMA-Tr(2)) tetraligand, which was efficiently deprotected and labelled with a 75% yield with technetium-99m, to obtain (99m)Tc-MAMA-CG. In mice, (99m)Tc-MAMA-CG was cleared mainly by the hepatobiliary system, resulting in a fast blood clearance. Brain uptake of (99m)Tc-MAMA-CG was low. Co-injection with the blood pool tracer iodine-125 human serum albumin ((125)I-HSA) demonstrated a brain/blood activity ratio for (99m)Tc-MAMA-CG that was significantly higher than that for (125)I-HSA (t test for dependent samples, P<0.02), indicating the ability of (99m)Tc-MAMA-CG to cross the blood-brain barrier. In vitro autoradiography demonstrated pronounced binding of (99m)Tc-MAMA-CG to beta-amyloid deposits in autopsy sections of the parietal and occipital cortex of an AD patient as compared with controls. Adding 10 microM Congo red during incubation displaced the binding of (99m)Tc-MAMA-CG. Congo red staining and autoradiography identified the same lesions. (99m)Tc-MAMA-CG seems to bind selectively to beta-amyloid deposition in human brain parenchyma and blood vessels in vitro and thus might be a lead compound for further development of a useful tracer agent for the in vivo diagnosis of Alzheimer's disease.
Authors:
N A Dezutter; R J Dom; T J de Groot; G M Bormans; A M Verbruggen
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of nuclear medicine     Volume:  26     ISSN:  0340-6997     ISO Abbreviation:  Eur J Nucl Med     Publication Date:  1999 Nov 
Date Detail:
Created Date:  2000-01-05     Completed Date:  2000-01-05     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  7606882     Medline TA:  Eur J Nucl Med     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  1392-9     Citation Subset:  IM    
Affiliation:
Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, K.U. Leuven, Leuven, Belgium.
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MeSH Terms
Descriptor/Qualifier:
Adult
Aged
Aged, 80 and over
Alzheimer Disease / radionuclide imaging*
Amyloid beta-Protein / analysis*
Animals
Benzoates / diagnostic use*
Biphenyl Compounds / diagnostic use
Brain / metabolism,  radionuclide imaging*
Coloring Agents / diagnostic use
Female
Humans
Isotope Labeling
Male
Mice
Mice, Inbred Strains
Middle Aged
Organotechnetium Compounds / diagnostic use*
Radiopharmaceuticals / diagnostic use
Technetium / diagnostic use
Tissue Distribution
Chemical
Reg. No./Substance:
0/99mTc-MAMA-chrysamine G; 0/Amyloid beta-Protein; 0/Benzoates; 0/Biphenyl Compounds; 0/Coloring Agents; 0/Organotechnetium Compounds; 0/Radiopharmaceuticals; 6472-91-9/chrysamine G; 7440-26-8/Technetium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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