Radiopharmaceuticals: Chemistry and Pharmacology (Drugs and the Pharmaceutical Sciences)

This timely resource compares single-photon emission tomography (SPECT), used mainly with Technetium and iodine for routine clinical examinations, and positron emission tomography (PET), employing short-lived radionuclides of carbon, oxygen, nitrogen, and fluorine in research investigations. Presenting the logic behind why one approach is better than another in various circumstances, Radiopharmaceuticals details the use of radiolabelled substrates in measuring the effect of disease and drugs on regional metabolism and receptor concentration/occupancy ... discusses factors affecting the selective retention of small metal complexes by various tissues ... analyzes the interaction of small exogenous metal complexes with enzymes in vivo and the critical role of stereochemistry ... explores the use of radiolabelled compounds in the study of neuroactive compounds, neurotransmitters, enzyme inhibitors, and substrates in vivo ... covers the design and pharmacology of radiolabelled drugs as probes of site of action, selectivity and specificity, and pharmacokinetics in vivo ... and more. Extensively referenced with over 1050 bibliographic citations, Radiopharmaceuticals is a state-of-the-art guide for pharmacists; organic, medicinal, and radiopharmaceutical chemists; pharmacokineticists; nuclear medicine physicians and technologists; neurochemists; and government regulatory personnel. Cover 1 Half Title 2 Title Page 6 Copyright Page 7 Preface 8 Contributors 14 Table of Contents 12 PERFUSION 16 1: Development of Positron Emitting Brain Perfusion Agents 16 2: Technetium-based Brain Perfusion Agents 52 3: Single Photon Radiopharmaceuticals for Imaging Myocardial Perfusion 112 4: Iodine Labeled Brain Perfusion Imaging Agents 156 RECEPTOR BINDERS 182 5: The Development of Single-photon Emitting Receptor-binding Radiotracers 182 6: Positron Emitting Tracers in Studies of Neurotransmission and Receptor Binding 236 7: Positron Emitter Labeled Enzyme Inhibitors and Substrates 286 8: The Pharmacology of Steroid Radiopharmaceuticals: Specific and Non-Specific Binding and Uptake Selectivity 316 9: The Influence of Structure Modification on the Metabolic Transformations of Radiolabeled Estrogen Derivatives 352 EXCRETION 384 10: Renal Radiopharmaceuticals 384 INDEX 450 The objective of this chapter is to review the development of positron-labeled brain perfusion agents.