[en] The overall objective during the period covered by this report was to develop a broad spectrum of radiopharmaceuticals labeled with short-lived cyclotron positron emitters, ¹¹C, ¹³N and ¹⁸F. The goals of the program during the last year were: (1) to complete the modular automated system for important precursor production - formaldehyde, methyliodide, cyanide; (2) to perform animal studies with the ¹⁸F-glucose analogues 2FDG and 3FDG and measure the constants for both agents in different animals; and (3) to initiate the development of new fatty acid analogues for the myocardial imaging and metabolism. As part of a collaboration with other groups seeking new agents for myocardium and brain, 9-/sup 123m/Te-telluriumheptadecanoic acid as a myocardial imaging agent was studied. This compound could be used for designing new fatty acid analogues labeled with ¹¹C and ¹⁸F that stay in the myocardium because of metabolic inhibition

[en] The overall objective during the period covered by this report was to develop a broad spectrum of radiopharmaceuticals labeled with short-lived cyclotron produced positron emitters, ¹¹C, ¹³N and ¹⁸F. The progress report of this year will summarize work done in the last three years. The goals of the program during the last three years were: to build and complete the transport system to Nuclear Medicine; to complete the modular automated system for important precursor production: formaldehyde, methyliodide, cyanide; to perform animal studies with the ¹⁸F-glucose analogs 2FDG and 3FDG and measure the rate constants and glucose metabolic rates derived from the Sokoloff model for both agents in different animal species; to initiate the development of new fatty acid analogs for myocardial imaging and metabolism; and to develop syntheses for ¹⁸F and ¹¹C sugar analogs

[en] A process is described for the production of /sup 18/F-2-deoxy-2-fluoro-D-glucose which comprises the steps of: (a) producing a compound; (b) reacting the resulting compound with a fluorinating agent in an inert organic solvent with heating at 100⁰C. to 150⁰C; and (c) hydrolyzing the resulting compounds to remove alkyl groups with BBr/sub 3/, BC1/sub 3/ or concentrated hydrochloric acid

[en] The structure localization relationship of a series of blood flow and metabolic tracers labeled with C-11 are discussed. The blood flow analogs are based on the structure of phentermine (α,α-dimethyl phenylethylamine). These agents were assessed for their uptake and retention in the brain of rats. The metabolic tracers are branched chain fatty acids. Their metabolic fate, in mice and preliminary quantitative metabolic data in dogs are presented

[en] The goal of radiopharmaceutical chemistry is to design and develop radiotracers targeted to an organ or function whose activity kinetics in tissue can be detected externally by a gamma or a positron device. Radiopharmaceuticals can be divided into the general categories of specific and non-specific agents. The specific radiopharmaceuticals are the tracers that follow a biochemical pathway or are involved in a particular interaction, for example metabolic substrates, drugs or analogs, and antibodies. Non-specific radiopharmaceuticals include radiolabeled liposomes, cells, microspheres, perfusion agents, inert gases, ethers, alcohols or thallium-201. The authors focus on trends in the design of specific agents. (Auth.)

[en] A new chemical route for the preparation of 2-[¹⁸F]fluoro-2-deoxy-D-glucose (2-¹⁸FDG) is discussed using anhydrous [¹⁸F]fluoride produced by the ²⁰Ne(d,α)¹⁸F reaction. The anhydous ¹⁸F^- is reacted with a previously prepared precursor, methyl 4,6-o-benzylidene-3-o-methyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranoside, in dimethyl formamide or hexamethylophosphoric triamide. The corresponding fluoro-deoxy-glucose derivative, upon treatment with borontribromide or concentrated hydrochloric acid, yields 2-¹⁸FDG in 10% (overall) yield. The substrate was characterized by thin-layer chromatography (TLC), and high-performance liquid chromatography (HPLC). Biodistribution studies were performed in mice, and imaging studies in dogs

[en] The goal of radiopharmaceutical chemistry is to design and develop radiotracers targeted to an organ or function whose activity kinetics in tissue can be detected externally by a gamma or a positron device. Radiopharmaceuticals are divided into the general categories of specific and non-specific agents. The specific radiopharmaceuticals are the tracers that follow a biochemical pathway or are involved in a particular interaction, for example metabolic substrates, drugs or analogs, and antibodies. This paper will focus on trends in the design of specific agents. The best radionuclides for the development of specific tracers are the positron emitting nuclides: carbon-11, nitrogen-13, oxygen-15 and fluorine-18. First the design of radiopharmaceuticals are considered in general (labeling strategies, stereochemical effects, specific activity). Next, a brief summary of the use of several radiopharmaceuticals is presented on the basis of their biochemical rationale. (orig./G.J.P.)

[en] The potential utility of Na¹⁸F for acute infarct imaging was assessed in a canine model with a positron camera. Transverse-section imaging of radiofluoride in five dogs with acute myocardial infarction, using a multicrystal positron camera, clearly demonstrated the zones of damage as areas of increased activity. The F-18 uptake in the infarct zones was found to peak at 48 to 72 hr after coronary ligation, as does Tc-99m pyrophosphate. Preliminary in vitro studies indicate that the relative F-18 uptake, 48 hr after ligation, is an inverse linear function of regional blood flow

[en] A number of new radiopharmaceuticals have been developed to increase the diagnostic utility of nuclear medicine in cardiac diseases. The radiochemistry and dosimetry of and clinical experience with these new agents are summarized, and are compared with more widely used methods for assessing myocardial perfusion (thallium-201 scintigraphy) and ventricular function (technetium-99m radioangiography). Emerging techniques for the evaluation of myocardial necrosis and metabolism are also presented, with emphasis on the use of radiolabeled antimyosin antibody and fatty acid analogue imaging in ischemic heart disease

[en] Brief item