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

Haofan Wang, Mrudula Pullambhatla, Tomas R. Guilarte, Ronnie Mease, Martin Gilbert Pomper

Research output: Contribution to journalArticle

Abstract

[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.

Original languageEnglish (US)
Pages (from-to)80-83
Number of pages4
JournalBiochemical and Biophysical Research Communications
Volume389
Issue number1
DOIs
StatePublished - Nov 6 2009

Fingerprint

Pneumonia
Inflammation
Imaging techniques
Radiopharmaceuticals
Rats
Autoradiography
Radioactivity
Theoretical Models
Lung
Animals
Proteins
N,N-diethyl-2-(2-(3-iodo-4-methoxyphenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidin-3-yl)acetamide
4-anisic acid
In Vitro Techniques

Keywords

  • Autoradiography
  • Peripheral benzodiazepine receptor
  • Pyrazolopyrimidine
  • Small animal imaging
  • Translocator protein

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Cell Biology
  • Molecular Biology

Cite this

Synthesis of [125I]iodoDPA-713 : A new probe for imaging inflammation. / Wang, Haofan; Pullambhatla, Mrudula; Guilarte, Tomas R.; Mease, Ronnie; Pomper, Martin Gilbert.

In: Biochemical and Biophysical Research Communications, Vol. 389, No. 1, 06.11.2009, p. 80-83.

Research output: Contribution to journalArticle

@article{c51008f74ea246cfad57ac7fcbf6b36c,
title = "Synthesis of [125I]iodoDPA-713: A new probe for imaging inflammation",
abstract = "[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.",
keywords = "Autoradiography, Peripheral benzodiazepine receptor, Pyrazolopyrimidine, Small animal imaging, Translocator protein",
author = "Haofan Wang and Mrudula Pullambhatla and Guilarte, {Tomas R.} and Ronnie Mease and Pomper, {Martin Gilbert}",
year = "2009",
month = "11",
day = "6",
doi = "10.1016/j.bbrc.2009.08.102",
language = "English (US)",
volume = "389",
pages = "80--83",
journal = "Biochemical and Biophysical Research Communications",
issn = "0006-291X",
publisher = "Academic Press Inc.",
number = "1",

}

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

AU - Pomper, Martin Gilbert

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

UR - http://www.scopus.com/inward/record.url?scp=70349155429&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=70349155429&partnerID=8YFLogxK

U2 - 10.1016/j.bbrc.2009.08.102

DO - 10.1016/j.bbrc.2009.08.102

M3 - Article

C2 - 19703411

AN - SCOPUS:70349155429

VL - 389

SP - 80

EP - 83

JO - Biochemical and Biophysical Research Communications

JF - Biochemical and Biophysical Research Communications

SN - 0006-291X

IS - 1

ER -