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Related Concept Videos

Positron Emission Tomography01:29

Positron Emission Tomography

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Positron emission tomography (PET) is a medical imaging technique involving radiopharmaceuticals — substances that emit short-lived radiation. Although the first PET scanner was introduced in 1961, it took 15 more years before radiopharmaceuticals were combined with the technique and revolutionized its potential.
One of the main requirements of a PET scan is a positron-emitting radioisotope, which is produced in a cyclotron and then attached to a substance used by the part of the body...
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Imaging Studies II: Positron Emission Tomography and Scintigraphy01:25

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Positron Emission Tomography (PET) is a medical imaging technique that provides crucial insights into the body's physiological functions at a molecular level. It is an indispensable resource for diagnosing, staging, and monitoring various illnesses, notably cancer, neurological disorders, and cardiovascular conditions.
Fundamental Principles of PET
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Related Experiment Video

Updated: Jun 25, 2025

Radiosynthesis, Quality Control, and Small Animal Positron Emission Tomography Imaging of 68Ga-Labelled Nano Molecules
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A Fast-Binding, Functionally Reversible, COX-2 Radiotracer for CNS PET Imaging.

Michael S Placzek1, Daniel K Wilton2, Michel Weïwer3

  • 1Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, United States.

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|May 27, 2024
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A new PET radiotracer, [11C]BRD1158, offers precise imaging of cyclooxygenase-2 (COX-2) in the brain. This tool reveals elevated COX-2 in Huntington

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Area of Science:

  • Neuroscience
  • Biochemistry
  • Radiochemistry

Background:

  • Cyclooxygenase-2 (COX-2) is implicated in central nervous system (CNS) disorders, but clinical data are inconsistent due to limited mechanistic understanding.
  • Developing specific positron emission tomography (PET) radiotracers for COX-2 is crucial for human neuroimaging and understanding its role in CNS pathology.

Purpose of the Study:

  • To develop and evaluate a novel, potent, selective, and fast-binding COX-2 PET radiotracer, [11C]BRD1158, for human neuroimaging.
  • To assess the utility of COX-2 as a biomarker in Huntington's disease (HD) models.

Main Methods:

  • Design and synthesis of [11C]BRD1158 prioritizing COX-2 potency, COX-1 selectivity, fast kinetics, and brain free fraction.
  • In vivo PET neuroimaging in rodent models with human COX-2 overexpression.
  • Analysis of post-mortem human HD brain samples and preclinical HD mouse models.

Main Results:

  • [11C]BRD1158 demonstrated high brain uptake, rapid target engagement, functional reversibility, and excellent specific binding in rodent models.
  • Elevated COX-2 levels were observed in disease-affected brain regions of HD patients and mouse models, predominantly in microglia.
  • [11C]BRD1158 showed high specificity and sensitivity for detecting COX-2 in vivo.

Conclusions:

  • [11C]BRD1158 is a promising PET radiotracer for human neuroimaging of COX-2.
  • COX-2 is a potential novel biomarker for Huntington's disease onset and progression.
  • The developed radiotracer facilitates mechanistic studies and clinical applications of COX-2 in CNS disorders.