Fluorine and Health

Fluorine and Health presents a critical multidisciplinary overview on the contribution of fluorinated compounds to resolve the important global issue of medicinal monitoring and health care. The involved subjects are organized in three thematic parts devoted to Molecular Imaging, Biomedical Materials and Pharmaceuticals. Initially the key-position of partially fluorinated low molecular weight compounds labelled either with the natural 19F-isotope for Magnetic Resonance Imaging (MRI) or labelled with the radioactive [18F]-isotope for Positron Emission Tomography (PET) is highlighted. Both non-invasive methods belong to the most challenging in vivo imaging techniques in oncology, neurology and in cardiology for the diagnosis of diseases having the highest mortality in the industrialized countries. The manifold facets of fluorinated biomaterials range from inorganic ceramics to perfluorinated organic molecules. Liquid perfluorocarbons are suitable for oxygen transport and as potential respiratory gas carriers, while fluorinated polymers are connected to the pathology of blood vessels. Another important issue concerns the application of highly fluorinated liquids in ophthalmology. Moreover, fluorine is an essential trace element in bone mineral, dentine and tooth enamel and is applied for the prophylaxis and treatment of dental caries. The various origins of human exposure to fluoride species is detailed to promote a better understanding of the effect of fluoride species on living organisms. Medicinally relevant fluorinated molecules and their interactions with native proteins are the main focus of the third part. New molecules fluorinated in strategic position are crucial for the development of pharmaceuticals with desired action and optimal pharmacological profile. Among the hundreds of marketed active drug components there are more than 150 fluorinated compounds. The chapters will illustrate how the presence of fluorine atoms alters properties of bioactive compounds at various biochemical steps, and possibly facilitate its emergence as pharmaceuticals. Finally the synthetic potential of a fluorinase, the first C-F bond forming enzyme, is summarized.

• New approach of topics involving chemistry, biology and medicinal techniques
• Transdisciplinar papers on fluoride products
• Importance of fluoride products in health
• Updated data on specific topics

Researchers in industry Scientists in academia Medical doctors PhD students

PART I: MOLECULAR IMAGING

1. Fluorine-18 Chemistry for Molecular Imaging with Positron Emission Tomography
   Frédéric Dollé, Dirk Roeda, Bertrand Kuhnast, and Marie-Claire Lasne

2. Application of 18F-PET Imaging for the Study of Alzheimer’s Disease
   Kjell Någren and Juha O. Rinne

3. 18F-Labeled PET-Tracers for Cardiological Imaging
   Klaus Kopka, Stefan Wagner, Michael Schäfers, Andreas Faust, Otmar Schober, and Günter Haufe

4. [18F]-Labeled PET and PET/CT Compounds in Oncology
   Ken Herrmann and Bernd Joachim Krause

5. Non-Invasive Physiology and Pharmacology Using 19F Magnetic Resonance
   Jian-Xin Yu, Weina Cui, Dawen Zhao, and Ralph P. Mason

PART II: BIOMEDICAL MATERIALS

1. Fluoride-Based Bioceramics
   Christian Rey, Christèle Combes, Christophe Drouet, and Hocine Sfihi

2. Fluoride in Dentistry and Dental Restoratives
   John W. Nicholson and Beata Czarnecka

3. Fluorinated Biomaterials for Cardiovascular Surgery
   Charles Baquey, Marie-Christine Durrieu, and Robert G. Guidoin

4. Fluorinated Molecules in Eye Surgery: Experimental and Clinical Benefit of a Heavy Silicone Oil Oxane Hd® (Mixture of Silicone Oil and RMN3 Fluorine Olefin) in the Treatment of Retinal Detachment
   I. Rico-Lattes, J. C. Quintyn, V. Pagot-Mathis, X. Benouaich, and A. Mathis

5. Biocompatibility of Highly Fluorinated Liquids Used in Ophthalmic Surgery
   Dirk-Henning Menz and Joachim H. Dresp

6. Perfluorochemical-Based Oxygen Therapeutics, Contrast Agents, and Beyond
   Marie Pierre Krafft and Jean G. Riess

7. Exposure of Humans to Fluorine and Its Assessment
   Maja Ponikvar

PART III: PHARMACEUTICALS

1. Biological Impacts of Fluorination: Pharmaceuticals Based on Natural Products
   Jean-Pierre Bégué and Danièle Bonnet-Delpon

2. Synthesis and Pharmacological Properties of Fluorinated Prostanoids
   Yasushi Matsumura

3. Synthesis and Biochemical Evaluation of Fluorinated Monoamine Oxidase Inhibitors
   Kenneth L. Kirk, Shinichi Yoshida, and Günter Haufe

4. Fluoroolefin Dipeptide Isosteres: Structure, Syntheses, and Applications
   John T. Welch

5. Molecular Interactions of Fluorinated Amino Acids in a Native Polypeptide Environment
   Mario Salwiczek, Christian Jäckel, and Beate Koksch

6. Biological Fluorination in Streptomyces cattleya: The Fluorinase
   Hai Deng, Fang-Lu Huang, James H. Naismith, David O′Hagan, Jonathan B. Spencer, and Xiaofeng Zhu