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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / chemical synthesis
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Acetamides / chemistry*
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Acetamides / pharmacokinetics
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Animals
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Brain / diagnostic imaging
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Female
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Inflammation / diagnostic imaging*
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Mice
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Mice, Inbred Strains
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Molecular Probes / chemical synthesis
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Molecular Probes / chemistry*
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Molecular Probes / pharmacokinetics
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Pneumonia / diagnostic imaging
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry*
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Pyrazoles / pharmacokinetics
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacokinetics
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / chemistry*
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Receptors, GABA / analysis*
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Receptors, GABA / metabolism
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Tomography, Emission-Computed
Substances
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Acetamides
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Molecular Probes
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N,N-diethyl-2-(2-(4-methoxyphenyl)-5,7-dimethyl-pyrazolo(1,5-a)pyrimidin-3-yl)-acetamide
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Pyrazoles
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Pyrimidines
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Radiopharmaceuticals
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Receptors, GABA
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TSPO protein, human
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N,N-diethyl-2-(2-(3-iodo-4-methoxyphenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidin-3-yl)acetamide