Source:http://linkedlifedata.com/resource/pubmed/id/17458949
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2007-5-10
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pubmed:abstractText |
Copper-64, a positron emitter suitable for positron emission tomography (PET), demonstrates improved in vivo clearance when chelated by the cross-bridged tetraazamacrocycle CB-TE2A compared to TETA. Good in vivo clearance was also observed for 64Cu-CB-TE2A conjugated to a peptide, which converts one coordinating carboxylate pendant arm to an amide. To better understand the in vivo stability of peptide- conjugated CB-TE2A, cross-bridged monoamides were synthesized. Crystal structures of natCu(II)-CB-TEAMA and natCu(II)-CB-PhTEAMA revealed hexadentate, distorted octahedral coordination geometry. In vivo biodistribution showed clearance of all 64Cu-radiolabeled cross-bridged monoamides from liver and bone marrow such that uptake at 24 h was <10% of uptake at 30 min. In contrast, >60% of 30 min uptake from 64Cu-TETA was retained in these tissues at 24 h. Clearance of 64Cu-cross-bridged monoamides from nontarget organs suggests good in vivo stability, thus supporting the use of CB-TE2A as a bifunctional chelator without modifications to the macrocycle backbone.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Chelating Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Copper Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Crown Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AndersonCarolyn JCJ,
pubmed-author:FiamengoAshley LAL,
pubmed-author:GolenJames AJA,
pubmed-author:PengYijieY,
pubmed-author:RheingoldArnold LAL,
pubmed-author:SouthwickEvan AEA,
pubmed-author:SpragueJennifer EJE,
pubmed-author:WeismanGary RGR,
pubmed-author:WongEdward HEH,
pubmed-author:WoodinKatrina SKS
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2527-35
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pubmed:dateRevised |
2007-12-3
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pubmed:meshHeading |
pubmed-meshheading:17458949-Amides,
pubmed-meshheading:17458949-Animals,
pubmed-meshheading:17458949-Chelating Agents,
pubmed-meshheading:17458949-Copper Radioisotopes,
pubmed-meshheading:17458949-Crown Compounds,
pubmed-meshheading:17458949-Crystallography, X-Ray,
pubmed-meshheading:17458949-Ligands,
pubmed-meshheading:17458949-Male,
pubmed-meshheading:17458949-Positron-Emission Tomography,
pubmed-meshheading:17458949-Radiopharmaceuticals,
pubmed-meshheading:17458949-Rats,
pubmed-meshheading:17458949-Rats, Inbred Lew,
pubmed-meshheading:17458949-Tissue Distribution
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis, characterization and in vivo studies of Cu(II)-64-labeled cross-bridged tetraazamacrocycle-amide complexes as models of peptide conjugate imaging agents.
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pubmed:affiliation |
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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