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Synthesis of [(125)I]iodoDPA-713: a new probe for imaging inflammation
Haofan Wang1, Mrudula Pullambhatla, Tomas R Guilarte
1Russell H. Morgan Department of Radiology and Radiological Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21231, USA.
[(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.
[(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.
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