Linked Life Data

12014963

Source:http://linkedlifedata.com/resource/pubmed/id/12014963

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
2002-5-16
pubmed:abstractText
syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC, 16 and 17), analogues of anti-1-amino-3-[18F]fluorocyclobutyl-1-carboxylic acid (FACBC), were prepared to evaluate the contributions of C-3 substitution and configuration on the uptake of these radiolabeled amino acids in a rodent model of brain tumors. Radiofluorinated targets [18F]16 and [18F]17 were prepared by no-carrier-added radiofluorination from their corresponding methanesulfonyl esters 12 and 13, respectively, with decay-corrected radiochemical yields of 30% for [18F]16 and 20% for [18F]17. In amino acid transport assays performed in vitro using 9L gliosarcoma cells, both [18F]16 and [18F]17 were substrates for L type amino acid transport, while [18F]17 but not [18F]16 was a substrate for A type transport. Biodistribution studies in normal Fischer rats with [18F]16 and [18F]17 showed high uptake of radioactivity (>2.0% dose/g) in the pancreas while other tissues studied, including liver, heart, lung, kidney, blood, muscle, and testis, showed relatively low uptake of radioactivity (<1.0% dose/g). In rats implanted intracranially with 9L gliosarcoma cells, the retention of radioactivity in tumor tissue was high at 5, 60, and 120 min after intravenous injection of [18F]16 and [18F]17 while the uptake of radioactivity in brain tissue contralateral to the tumor remained low (<0.3% dose/g). Ratios of tumor uptake to normal brain uptake for [18F]16 were 7.5:1, 7:1, and 5:1 at 5, 60, and 120 min, respectively, while for [18F]17 the ratios were 7.5:1, 9:1, and 9:1 at the same time points. This work demonstrates that like anti-[18F]FACBC, [18F]16 and [18F]17 are excellent candidates for imaging brain tumors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
23
pubmed:volume
45
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2250-9
pubmed:dateRevised
2003-11-14
pubmed:meshHeading
pubmed-meshheading:12014963-Amino Acid Transport System A, pubmed-meshheading:12014963-Amino Acid Transport System L, pubmed-meshheading:12014963-Amino Acids, pubmed-meshheading:12014963-Animals, pubmed-meshheading:12014963-Brain, pubmed-meshheading:12014963-Brain Neoplasms, pubmed-meshheading:12014963-Carboxylic Acids, pubmed-meshheading:12014963-Crystallography, X-Ray, pubmed-meshheading:12014963-Cyclobutanes, pubmed-meshheading:12014963-Fluorine Radioisotopes, pubmed-meshheading:12014963-Gliosarcoma, pubmed-meshheading:12014963-Isotope Labeling, pubmed-meshheading:12014963-Ligands, pubmed-meshheading:12014963-Male, pubmed-meshheading:12014963-Neoplasm Transplantation, pubmed-meshheading:12014963-Propionic Acids, pubmed-meshheading:12014963-Radiopharmaceuticals, pubmed-meshheading:12014963-Rats, pubmed-meshheading:12014963-Rats, Inbred F344, pubmed-meshheading:12014963-Stereoisomerism, pubmed-meshheading:12014963-Tissue Distribution, pubmed-meshheading:12014963-Tomography, Emission-Computed, pubmed-meshheading:12014963-Tumor Cells, Cultured
pubmed:year
2002
pubmed:articleTitle
Synthesis of syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC), potential PET ligands for tumor detection.
pubmed:affiliation
Emory Center for Positron Emission Tomography, Department of Radiology, Emory University, 1364 Clifton Road, Northeast, Atlanta, Georgia 30322, USA.
pubmed:publicationType
Journal Article