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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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Radiological Investigation III: Pulmonary Angiogram and PET Scan01:13

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Radiological investigations are paramount in the diagnosis and management of various pulmonary diseases. Two essential investigations are the Pulmonary Angiogram and the Positron Emission Tomography (PET) Scan.
Pulmonary Angiogram
A Pulmonary Angiogram is an invasive procedure involving injecting a contrast medium through a catheter threaded into the pulmonary artery or the right side of the heart to visualize the pulmonary vasculature. Computed Tomography (CT) scans have mainly replaced this...
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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.
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Updated: Jan 18, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging
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PET radiotracer targeting the complement C3a receptor.

Ravi Naik1, Hyojin Cha1, Fangyi Shen1

  • 1The Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD, USA.

Nuclear Medicine and Biology
|September 10, 2025
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Summary
This summary is machine-generated.

Researchers developed a novel PET radiotracer targeting the C3a receptor (C3aR) for imaging neuroinflammation. While feasible, the tracer showed suboptimal specificity and kinetics, necessitating further optimization for clinical use.

Keywords:
C3aRComplement component receptorsNeuroinflammationPET

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Area of Science:

  • Neuroscience
  • Immunology
  • Radiochemistry

Background:

  • Positron-emission tomography (PET) imaging offers insights into innate immunity in CNS diseases.
  • Targeting the complement system, specifically the C3a receptor (C3aR), is crucial for understanding neuroinflammation and drug development.

Purpose of the Study:

  • To develop a novel PET radiotracer for specific in vivo imaging of the C3a receptor (C3aR).
  • To evaluate the feasibility of C3aR PET imaging in a neuroinflammation model.

Main Methods:

  • One-step synthesis of the C3aR radiotracer [18F]1.
  • Ex vivo imaging studies in mice, including control and lipopolysaccharide (LPS)-induced neuroinflammation models.
  • Blocking experiments to determine tracer specificity and binding kinetics.

Main Results:

  • [18F]1 was successfully radiolabeled with high purity (>95%) and moderate molar activity (~155 GBq/μmol).
  • In control mice, [18F]1 exhibited high brain uptake with predominantly non-specific binding (18% specific).
  • In LPS-treated mice, brain uptake of [18F]1 increased (~2-fold), with partially specific binding (43%) to C3aR, but demonstrated high non-specific binding and slow kinetics.

Conclusions:

  • The study demonstrated the feasibility of developing a PET radiotracer for C3aR imaging in neuroinflammation.
  • [18F]1 is suboptimal due to insufficient specific binding, high non-specific binding, and slow kinetics.
  • Future research should focus on developing optimized C3aR PET tracers with improved characteristics.