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Title: Synthesis of [(125)I]iodoDPA-713: a new probe for imaging inflammation.

Authors: Wang, Haofan; Pullambhatla, Mrudula; Guilarte, Tomas R; Mease, Ronnie C; Pomper, Martin G

Published In Biochem Biophys Res Commun, (2009 Nov 06)

Abstract: [(125)I]IodoDPA-713 [(125)I]1, which targets the translocator protein (TSPO, 18 kDa), was synthesized in seven steps from methyl-4-methoxybenzoate as a tool for quantification of inflammation in preclinical models. Preliminary in vitro autoradiography and in vivo small animal imaging were performed using [(125)I]1 in a neurotoxicant-treated rat and in a murine model of lung inflammation, respectively. The radiochemical yield of [(125)I]1 was 44+/-6% with a specific radioactivity of 51.8 GBq/micromol (1400 mCi/micromol) and >99% radiochemical purity. Preliminary studies showed that [(125)I]1 demonstrated increased specific binding to TSPO in a neurotoxicant-treated rat and increased radiopharmaceutical uptake in the lungs of an experimental inflammation model of lung inflammation. Compound [(125)I]1 is a new, convenient probe for preclinical studies of TSPO activity.

PubMed ID: 19703411 Exiting the NIEHS site

MeSH Terms: Acetamides/chemical synthesis; Acetamides/chemistry*; Acetamides/pharmacokinetics; Animals; Brain/diagnostic imaging; Female; Inflammation/diagnostic imaging*; Mice; Mice, Inbred Strains; Molecular Probes/chemical synthesis; Molecular Probes/chemistry*; Molecular Probes/pharmacokinetics; Pneumonia/diagnostic imaging; Pyrazoles/chemical synthesis; Pyrazoles/chemistry*; Pyrazoles/pharmacokinetics; Pyrimidines/chemical synthesis; Pyrimidines/chemistry*; Pyrimidines/pharmacokinetics; Radiopharmaceuticals/chemical synthesis; Radiopharmaceuticals/chemistry*; Radiopharmaceuticals/pharmacokinetics; Rats; Receptors, GABA/analysis*; Receptors, GABA/metabolism; Tomography, Emission-Computed

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