Preliminary Evaluations of [C]Verubulin: Implications for Microtubule Imaging With PET.

TitlePreliminary Evaluations of [C]Verubulin: Implications for Microtubule Imaging With PET.
Publication TypeJournal Article
Year of Publication2021
AuthorsLindberg A, Mossine AV, Aliaga A, Hopewell R, Massarweh G, Rosa-Neto P, Shao X, Bernard-Gauthier V, Scott PJH, Vasdev N
JournalFront Neurosci
Volume15
Pagination725873
Date Published2021
ISSN1662-4548
Abstract

[C]Verubulin (a.k.a.[C]MCP-6827), [C]HD-800 and [C]colchicine have been developed for imaging microtubules (MTs) with positron emission tomography (PET). The objective of this work was to conduct an comparison of [C]verubulin for MT imaging in mouse and rat brain, as well as an study with this radiotracer in rodent and human Alzheimer's Disease tissue. Our preliminary PET imaging studies of [C]verubulin in rodents revealed contradictory results between mouse and rat brain uptake under pretreatment conditions. autoradiography with [C]verubulin showed an unexpected higher uptake in AD patient tissue compared with healthy controls. We also conducted the first comparative PET imaging study with [C]verubulin, [C]HD-800 and [C]colchicine in a non-human primate. [C]Verubulin and [C]HD-800 require pharmacokinetic modeling and quantification studies to understand the role of how these radiotracers bind to MTs before translation to human use.

DOI10.3389/fnins.2021.725873
Alternate JournalFront Neurosci
PubMed ID34566568
PubMed Central IDPMC8456034