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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.
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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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Synthesis, Radiochemistry, and Preclinical Assessment of the First GPR39 PET Imaging Agent.

Bhuvanachandra Bhoopal1, Krishna Kumar Gollapelli1, Naresh Damuka1

  • 1Department of Radiology, Wake Forest School of Medicine, Winston-Salem, North Carolina 27157, United States.

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|March 19, 2026
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Researchers developed the first radiotracer, [11C]TMN-OMe, to quantify GPR39 levels in vivo. This novel imaging tool aids in understanding GPR39

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Area of Science:

  • Neuroscience
  • Radiochemistry
  • Medical Imaging

Background:

  • GPR39, a zinc-sensing G protein-coupled receptor, plays crucial roles in neurophysiological and metabolic functions.
  • Altered GPR39 levels are implicated in neurodegenerative diseases like Alzheimer's disease (AD).
  • In vivo quantification of GPR39 is essential for understanding its role in disease and for drug development.

Purpose of the Study:

  • To develop and evaluate the first radiotracer for in vivo GPR39 imaging.
  • To assess the feasibility of using [11C]TMN-OMe for quantifying GPR39 levels in preclinical models.

Main Methods:

  • Synthesis and radiolabeling of [11C]TMN-OMe.
  • Preclinical evaluation including radiochemical purity, molar activity, and stability assessments.
  • In vivo microPET/CT imaging, biodistribution studies, and autoradiography in wild-type, GPR39 knockout, and AD mouse models.

Main Results:

  • [11C]TMN-OMe demonstrated high radiochemical purity, molar activity, and stability.
  • In vivo imaging confirmed selective binding to GPR39.
  • Significantly reduced brain uptake of [11C]TMN-OMe was observed in GPR39 knockout mice, AD mice, and under blockade conditions.

Conclusions:

  • The developed radiotracer [11C]TMN-OMe is suitable for quantifying GPR39 levels in vivo.
  • GPR39-based imaging represents a novel platform for studying mechanistic changes in neurological disorders.
  • This imaging approach holds potential for drug development and treatment monitoring in neurodegenerative diseases.