title: PET radiotracers for imaging P-glycoprotein: the challenge for early diagnosis in AD.
abstract: PET radiotracer development to target in vivo P-glycoprotein (P-gp) could be an important strategy for the early diagnosis of neurodegenerative disorders such as Alzheimer's disease (AD). Indeed, as a dysfunction of P-gp is responsible for the accumulation of β-amyloid plaques (a hallmark of AD) in brain parenchyma, P-gp is the cause of AD onset. P-gp substrates and inhibitors are useful for imaging the activity or expression of this protein, respectively; herein we discuss the in vivo evaluation of some ¹¹C radiotracers with P-gp-inhibitory activity, such as [¹¹C]MC18 and [¹¹C]MC113, as well as P-gp substrates [¹¹C]MC266 and [¹¹C]MC80. Moreover, the radiosynthesis of all these P-gp probes is reported.
authors.affiliation: Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari "Aldo Moro" via Orabona 4, 70125 Bari (Italy); BIOFORDRUG s.r.l., Spin-off, Università degli Studi di Bari "Aldo Moro" via Orabona 4, 70125 Bari (Italy).
authors.forename: Marcello
authors.initials: M
authors.lastname: Leopoldo
authors.forename: Marialessandra
authors.initials: M
authors.lastname: Contino
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
authors.forename: Nicola Antonio
authors.initials: NA
authors.lastname: Colabufo
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000544:Alzheimer Disease / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000378:metabolism; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D002250:Carbon Radioisotopes / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals
keywords: Alzheimer’s disease; P-glycoprotein; PET radiotracers; early diagnosis