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    Bioorg Med Chem Lett. 2008 Feb 15;18(4):1264-8. Epub 2008 Jan 13.

    Synthesis and evaluation of [123I] labeled iodovinyl amino acids syn-, anti-1-amino-3-[2-iodoethenyl]-cyclobutane-1-carboxylic acid, and 1-amino-3-iodomethylene-cyclobutane-1-carboxylic acid as potential SPECT brain tumor imaging agents.

    Yu W, Williams L, Malveaux E, Camp VM, Olson JJ, Goodman MM.

    Source

    Department of Radiology, Emory University, School of Medicine, Atlanta, GA 30322, USA.

    Abstract

    syn- and anti-1-amino-3-[2-iodoethenyl]-cyclobutane-1-carboxylic acid (syn-, anti-IVACBC 16, 17) and their analogue 1-amino-3-iodomethylene-cyclobutane-1-carboxylic acid (gem-IVACBC 18) were synthesized and radioiodoinated with [(123)I] in 34-43% delay-corrected yield. All these amino acids entered 9L gliosarcoma cells primarily via L-type transport in vitro with high uptake of 8-10% ID/1 x 10(6) cells. Biodistribution studies of [(123)I]16, 17 and 18 in rats with 9L gliosarcoma brain tumors demonstrated high tumor to brain ratios (4.7-7.3:1 at 60 min post-injection). In this model, syn-, anti-, and gem-[(123)I]IVACBC are promising radiotracers for SPECT brain tumor imaging.

    PMID:
    18258425
    [PubMed - indexed for MEDLINE]
    PMCID: PMC2362394
    Free PMC Article

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