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Scott, Peter J. H. Radiochemical Syntheses, Radiopharmaceuticals for Positron Emission Tomography eBook

Radiochemical Syntheses, Radiopharmaceuticals for Positron Emission Tomography

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eBook Publisher: John Wiley & Sons
Imprint: Wiley

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The ultimate reference guide to the synthesis of radiopharmaceuticals

The Radiochemical Syntheses series provides scientists and professionals with a comprehensive reference to proven synthetic methods for radiochemical reactions, along with step-by-step guidance on how to replicate these syntheses in the laboratory.

Volume 1 in the series focuses on the synthesis and purification of radiopharmaceuticals in clinical use today. It brings together in one complete, self-contained volume a collection of monographs containing a wealth of practical information from across the literature, demonstrating in meticulous detail how to prepare radiopharmaceuticals for positron emission tomography (PET) imaging, especially in tumor studies, cardiology, and neuroscience.

Readers have key experimental details culled from the literature at their fingertips, greatly simplifying the process of qualifying a site for the clinical production of new radiopharmaceuticals.

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Title of eBook: Radiochemical Syntheses, Radiopharmaceuticals for Positron Emission Tomography
Release Date: 12-28-2011
Publisher: Wiley

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Parent title Radiochemical Syntheses,...
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Radiochemical Syntheses, Radiopharmaceuticals for Positron Emission Tomography


Chapter One

SYNTHESIS OF [18F]-FLUORODEOXYGLUCOSE ([18F]FDG)

Michelle L. Richards and Peter J. H. Scott

Department of Radiology, University of Michigan School of Medicine, Ann Arbor, Michigan

1 INTRODUCTION

Positron emission tomographic (PET) imaging provides a noninvasive, accurate diagnostic method of imaging and detecting possible diseases at a cellular, molecular, and tissue level. PET has a proportional relationship between the tissue intensity on the tomographic image and the actual radiopharmaceutical concentration in tissue. [18F]Fluorodeoxyglucose ([18F]FDG) is a glucose analog and is known as the "work horse" of PET simply because of the multiple modalities for application. The implications of abnormal glucose metabolism are vital in evaluating a variety of diseases, and the applications of this positron emitting radiotracer are great. [18F]FDG is preferentially taken up into cells with high metabolic activity by specific glucose transporters (GluT) and phosphorylated by hexokinase. It becomes metabolically trapped in the cell because [18F]FDG-6-phosphate is not a substrate for glucose-6-phosphate isomerase, the enzyme that metabolizes glucose, and therefore cannot be broken down. During radioactive decay, 18F decays to 18O, allowing the decayed product, 2-18O-deoxyglucose-6-phosphate, to enter the normal glucose metabolic pathway.

The first synthesis of [18F]FDG was based on a direct electrophilic substitution reaction by Wolf et al. in 1976. This fluorination reaction by electrophilic substitution refers to the addition of fluor

...

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