Positron-Emitting Radiopharmaceuticals

Provide an overview of radionuclides with relevant applications in PET.

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Positron-Emitting Radiopharmaceuticals Piero A. Salvadori, Elena Filidei, and Assuero Giorgetti

Contents 3.1    Section I: Positron-Emitting Radionuclides and Labeling Strategies 3.1.1   Positron-Emitting Radionuclides and Basic Chemistry 3.1.2   Substrate Characteristics and Radiolabeling Strategies 3.1.3   Radiopharmaceuticals and Biological Systems 3.1.4   Production Flowchart and Related Issues 3.1.5   Basic of Automation and Synthesis Devices 3.1.6   18F-Labeled Radiopharmaceuticals 3.1.7   11C-Labeled Radiopharmaceuticals 3.1.8   68Ga-Labeled and Radiometal-Based Radiopharmaceuticals 3.1.9   Miscellanea 3.1.10  What Might Be Next



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3.2    Section II: Positron-Emitting Radiopharmaceuticals for Clinical Use 3.2.1   Sodium 18F-Fluoride 3.2.2   Flow/Perfusion Agents 3.2.3   Energy Substrates 3.2.4   Substrates for Phospholipid Synthesis 3.2.5   Substrates for Protein Synthesis 3.2.6   Substrates for DNA Synthesis 3.2.7   Positron-Emitting Agents Based on Ligand-Acceptor Interaction 3.2.8   Amyloid Imaging Agents 3.2.9   Tissue Hypoxia Imaging Agents 3.2.10  Neoangiogenesis Imaging Agents 3.2.11  Apoptosis Imaging Agents

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Further Reading

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Learning Objectives

• Provide an overview of radionuclides with relevant applications in PET. • Define structure-activity relationships and how radiolabeling can induce molecular/biological perturbation. • Describe routes of administration and their impact on biodistribution. P. A. Salvadori (*) PET/Cyclotron Unit, CNR Institute of Clinical Physiology, Pisa, Italy e-mail: [email protected] E. Filidei · A. Giorgetti Nuclear Medicine Unit, Fondazione CNR/Regione Toscana Gabriele Monasterio, Pisa, Italy

• Describe the impact of molecular size, polarity, and functional groups on distribution. • Summarize key issues on handling positron-emitting radionuclides (shielding) and radiochemical synthesis. • Explain main advantages and issues regarding 11C-labeled radiopharmaceuticals. • Provide basic information on 68Ga-labeled radiopharmaceuticals and the 68Ge/68Ga generator. • Provide basic information on the synthesis and use of 124 I-labeled radiopharmaceuticals. • Provide information on the rationale for using positronemitting radiopharmaceuticals in different pathophysiologic conditions according to the biologic/metabolic event targeted by different classes of imaging agents.

© Springer Nature Switzerland AG 2019 D. Volterrani et al. (eds.), Nuclear Medicine Textbook, https://doi.org/10.1007/978-3-319-95564-3_3

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3.1

P. A. Salvadori et al.

 ection I: Positron-Emitting S Radionuclides and Labeling Strategies

Imaging with positron emission tomography (PET) is based on the detection of the annihilation radiation. Annihilation radiation occurs when matter is converted to energy. This phenomenon occurs when a negatively charged electron (negatron) and a positively charged electron (positron, emitted in the course of decay o