AUTHOR=Lindberg Anton , Mossine Andrew V. , Aliaga Arturo , Hopewell Robert , Massarweh Gassan , Rosa-Neto Pedro , Shao Xia , Bernard-Gauthier Vadim , Scott Peter J. H. , Vasdev Neil 

TITLE=Preliminary Evaluations of [11C]Verubulin: Implications for Microtubule Imaging With PET

JOURNAL=Frontiers in Neuroscience

VOLUME=15

YEAR=2021

URL=https://www.frontiersin.org/journals/neuroscience/articles/10.3389/fnins.2021.725873

DOI=10.3389/fnins.2021.725873

ISSN=1662-453X

ABSTRACT=<p>[<sup>11</sup>C]Verubulin (a.k.a.[<sup>11</sup>C]MCP-6827), [<sup>11</sup>C]HD-800 and [<sup>11</sup>C]colchicine have been developed for imaging microtubules (MTs) with positron emission tomography (PET). The objective of this work was to conduct an <italic>in vivo</italic> comparison of [<sup>11</sup>C]verubulin for MT imaging in mouse and rat brain, as well as an <italic>in vitro</italic> study with this radiotracer in rodent and human Alzheimer’s Disease tissue. Our preliminary PET imaging studies of [<sup>11</sup>C]verubulin in rodents revealed contradictory results between mouse and rat brain uptake under pretreatment conditions. <italic>In vitro</italic> autoradiography with [<sup>11</sup>C]verubulin showed an unexpected higher uptake in AD patient tissue compared with healthy controls. We also conducted the first comparative <italic>in vivo</italic> PET imaging study with [<sup>11</sup>C]verubulin, [<sup>11</sup>C]HD-800 and [<sup>11</sup>C]colchicine in a non-human primate. [<sup>11</sup>C]Verubulin and [<sup>11</sup>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.</p>