Synthesis of [{sup 125}I]iodoDPA-713: A new probe for imaging inflammation

Journal Article · Fri Nov 06 00:00:00 EST 2009 · Biochemical and Biophysical Research Communications

DOI:https://doi.org/10.1016/J.BBRC.2009.08.102· OSTI ID:22199861

Wang, Haofan; Pullambhatla, Mrudula ^[1]; Guilarte, Tomas R. ^[2]; Mease, Ronnie C. ^[1]

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1. Russell H. Morgan Department of Radiology and Radiological Sciences, Johns Hopkins Medical Institutions, 1550 Orleans Street, Baltimore, MD 21231 (United States)
2. Department of Environmental Health Sciences, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD 21205 (United States)

[{sup 125}I]IodoDPA-713 [{sup 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 [{sup 125}I]1 in a neurotoxicant-treated rat and in a murine model of lung inflammation, respectively. The radiochemical yield of [{sup 125}I]1 was 44 {+-} 6% with a specific radioactivity of 51.8 GBq/{mu}mol (1400 mCi/{mu}mol) and >99% radiochemical purity. Preliminary studies showed that [{sup 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 [{sup 125}I]1 is a new, convenient probe for preclinical studies of TSPO activity.

• OSTI ID: 22199861
• Journal Information: Biochemical and Biophysical Research Communications, Vol. 389, Issue 1; Other Information: Copyright (c) 2009 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.; Country of input: International Atomic Energy Agency (IAEA); ISSN 0006-291X
• Country of Publication: United States
• Language: English

Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRONMENTAL POLLUTANT EFFECTS ON LIVING ORGANISMS AND BIOLOGICAL MATERIALS
ACETAMIDE
AUTORADIOGRAPHY
IMPURITIES
IN VITRO
IN VIVO
INFLAMMATION
IODINE 125
LUNGS
RADIOACTIVITY
RADIOCHEMISTRY
RADIOPHARMACEUTICALS
RATS
RECEPTORS
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
SYNTHESIS