title: Positron emission tomography radioligands for in vivo imaging of Aβ plaques.
abstract: The development of positron emission tomography (PET) radioligands for the non-invasive imaging of amyloid-β plaque burden has been the focus of intense research efforts over the last decade. A variety of structural backbones have been investigated and several radiolabeled molecules have been evaluated in phase I (and later) clinical studies. These efforts have been driven by the desire not only to develop a suitable diagnostic imaging agent but also to develop a means to evaluate potential therapies for Alzheimer's disease. This review focuses on the development of these ligands, as well as the radiochemistry and current regulatory status of these PET radioligands. Particular attention is given to those ligands that have progressed to the later stages of drug development (phase II/III clinical trial studies) or approved New Drug Application status.
authors.affiliation: Departments of Radiology, University of Pittsburgh, Pittsburgh, PA, 15213, USA.
authors.forename: N Scott
authors.initials: NS
authors.lastname: Mason
authors.forename: Chester A
authors.initials: CA
authors.lastname: Mathis
authors.forename: William E
authors.initials: WE
authors.lastname: Klunk
mesh_terms: D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D001921:Brain / Q000000981:diagnostic imaging*; D002250:Carbon Radioisotopes / Q000737:chemistry; D005026:Ethylene Glycols / Q000138:chemical synthesis* / Q000494:pharmacology; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D008024:Ligands; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology; D013267:Stilbenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D016229:Amyloid beta-Peptides; D000814:Aniline Compounds; D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D005026:Ethylene Glycols; D005462:Fluorine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D013267:Stilbenes; C581552:flutemetamol; C545186:florbetapir; C527756:4-(N-methylamino)-4'-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)stilbene
keywords: Aβ plaques; PET; amyloid; florbetaben; florbetapir; flutemetamol