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Review

Fluorinated molecules in the diagnosis and treatment of neurodegenerative diseases

    Boyenoh Gaye

    Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, University of the Sciences in Philadelphia, PA 19104, USA.

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    Email the corresponding author at a.adejar@usp.edu

    &
    Adeboye Adejare

    † Author for correspondence

    Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, University of the Sciences in Philadelphia, PA 19104, USA.

    Search for more papers by this author

    Email the corresponding author at a.adejar@usp.edu

    Published Online:19 Aug 2009https://doi.org/10.4155/fmc.09.85

    Abstract

    The use of fluorinated molecules as drugs and imaging agents for CNS disorders has been studied extensively over the years. Incorporating a fluorine atom into the structure of a drug changes its physiochemical properties and can thereby lead to much more desirable pharmacokinetic and pharmacodynamic properties. This change can help to facilitate blood–brain barrier permeability, which is a critical matter for drugs intended for CNS activities. Fluorine incorporation into structures of drugs for the treatment of neurodegenerative diseases has been an attractive field for drug discovery. Such incorporation can greatly influence the physicochemical properties, metabolic stability and receptor binding affinity of the resulting molecule. Some studies have shown that when a proton was substituted with fluorine, the binding or inhibitory potency was greatly increased. The fluorine-18 isotope, 18F, is utilized in detection and diagnosis of neurodegenerative diseases, whereas 19F compounds are used in the treatment of these diseases and in MRI. 18F is widely used in PET imaging because it offers the advantage of a longer half-life compared with other radionuclides. It is used for imaging various receptors and transporters that have been linked to neurodegenerative diseases, such as Alzheimer’s disease, Parkinson’s disease, Huntington’s disease and multiple system atrophy. Fluorine plays an important role in the diagnosis and treatment of many CNS diseases, including neurodegenerative disorders. The use of fluorine in the diagnosis and treatment of neurodegenerative diseases, such as Alzheimer’s disease and Parkinson’s disease, will be discussed in this review.

    Papers of special note have been highlighted as: ▪▪ of considerable interest

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