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The radiolabeling of an organic compound is perhaps the simplest and oldest technique in radiotracer design, in which labeling is commonly done using positron emission tomography (PET) radionuclides, including 11C, 13N, and 18F. In recent decades, radiofluorination of various molecules and peptides, such as somatostatin and neurotensin, has been considered for use in imaging. In this chapter, we summarize the 18F-labeled heterocycles that are used as targeted radiopharmaceuticals and imaging agents. Many heterocyclic backbones have been 18F-labeled, including imidazoles, pyrrolidines, triazole-functionalized peptides, triazoles, benzothiazoles, pyridines, quinolines, and β-carbolines, to image and detect various disorders and diseases, including cancerous cells, distant metastases, Alzheimer’s disease, Parkinson’s disease, schizophrenia, and inflammation.

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