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Toxic epibatidine was structurally modified to image Alzheimer´s disease

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Toxic epibatidine was structurally modified to image Alzheimer´s disease
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Abstract
The video describes the process of the development of a radiopharmaceutical for imaging of Alzheimer´s disease with positron emission tomography. The toxin epibatidine, which was originally derived from a poison arrow frog, is known to bind to various subtypes of nicotinic acetylcholine receptors. Those with an alpha1 subunit are mainly responsible for the toxic action, those with alpha4 and alpha7 subunits are important for Alzheimer´s disease. Structural modification allowed avoidance of the toxic action. The new molecule, called flubatine, contains fluorine in 6-position of a pyridine which was exchanged by the cyclotron-produced positron emitter fluorine-18. Successful in vitro and preclinical in vivo characterization of the radiolabelled flubatine allowed radiopharmaceutical production and use of the compound for PET imaging of patients with Alzheimer´s disease.
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