ABSTRACT

CONTENTS 4.1 Overview . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 96 4.2 Molecular Target Selection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 97 4.3 Tracer Molecule . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 98 4.4 Radionuclide Selection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 100 4.5 Labeling Position . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 102 4.6 Radiosynthesis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 103 4.7 PET Nuclides: Reactions and Radiopharmaceuticals . . . . . . . . . . . 104

4.7.1 Carbon-11 . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 104 4.7.2 Fluorine-18 . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 105

4.7.2.1 Deoxyglucose Method . . . . . . . . . . . . . . . . . . . . . . 106 4.8 SPECT Radionuclides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 108

4.8.1 Technetium-99m: Production, Coordination Chemistry, and Radiopharmaceuticals . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109

4.8.2 Gallium and Indium: Radioisotopes and Their Coordination Chemistry . . . . . . . . . . . . . . . . . . . . . . . . . . . 115 4.8.2.1 Gallium and Indium Ligands . . . . . . . . . . . . . . . . . 116 4.8.2.2 Gallium and Indium Radiopharmaceuticals . . . . . . 118

4.8.3 Copper Radioisotopes and Copper Coordination Chemistry . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 120

4.9 Monoclonal Antibodies and Peptides in Molecular Imaging . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 121 4.9.1 Monoclonal Antibodies . . . . . . . . . . . . . . . . . . . . . . . . . . . . 121 4.9.2 Peptides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 122

4.10 Radiopharmaceutical Quality Control: Radiochemical Purity, Specific Activity, and Radiolysis . . . . . . . . . . . . . . . . . . . . . . . . . . . 125

4.11 Advances in Radiopharmaceutical Development and New Trends in Radiochemistry . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 125

References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 126 Further Reading . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 132

One of the bases of NM is the ability to produce molecules that are capable of acting as selective markers for the biophysical, biochemical, or pharmacological processes that are of interest. Over recent decades, thousands of molecules have been labeled with emitting nuclides for studying more than a hundred different processes in the human body. The unparalleled ability of these molecules to depict in vivo metabolic pathways and interactions has led to the development of a new scientific area: molecular imaging. In this chapter, we will describe the main questions related to the use of radiopharmaceuticals in molecular imaging studies and indicate some of their principal applications in clinical and research studies.