TY - JOUR
T1 - Synthesis of [125I]iodoDPA-713
T2 - A new probe for imaging inflammation
AU - Wang, Haofan
AU - Pullambhatla, Mrudula
AU - Guilarte, Tomas R.
AU - Mease, Ronnie C.
AU - Pomper, Martin G.
N1 - Funding Information:
We thank Jennifer McGlothan for expertise in autoradiography and James Fox and Gilbert Green for providing the in vivo images. We also thank the Dana Foundation and NIH Grants CA92871 and ES07062 for financial support. The funding sources had no impact on the scientific content of this contribution.
PY - 2009/11/6
Y1 - 2009/11/6
N2 - [125I]IodoDPA-713 [125I]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 [125I]1 in a neurotoxicant-treated rat and in a murine model of lung inflammation, respectively. The radiochemical yield of [125I]1 was 44 ± 6% with a specific radioactivity of 51.8 GBq/μmol (1400 mCi/μmol) and >99% radiochemical purity. Preliminary studies showed that [125I]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 [125I]1 is a new, convenient probe for preclinical studies of TSPO activity.
AB - [125I]IodoDPA-713 [125I]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 [125I]1 in a neurotoxicant-treated rat and in a murine model of lung inflammation, respectively. The radiochemical yield of [125I]1 was 44 ± 6% with a specific radioactivity of 51.8 GBq/μmol (1400 mCi/μmol) and >99% radiochemical purity. Preliminary studies showed that [125I]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 [125I]1 is a new, convenient probe for preclinical studies of TSPO activity.
KW - Autoradiography
KW - Peripheral benzodiazepine receptor
KW - Pyrazolopyrimidine
KW - Small animal imaging
KW - Translocator protein
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U2 - 10.1016/j.bbrc.2009.08.102
DO - 10.1016/j.bbrc.2009.08.102
M3 - Article
C2 - 19703411
AN - SCOPUS:70349155429
SN - 0006-291X
VL - 389
SP - 80
EP - 83
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
IS - 1
ER -