Pharmacokinetic Modeling of [¹¹C]GSK-189254, PET Tracer Targeting H₃ Receptors, in Rat Brain.

ABSTRACT: The histamine H₃ receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H₃ receptor antagonist [¹¹C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H₃ receptor density in animal models of neurodegenerative disease. [¹¹C]GSK-189254 was intravenously administered to healthy Wistar rats (n = 10), and a 60 min dynamic PET scan was carried out. Arterial blood samples were obtained during the scan to generate a metabolite-corrected plasma input function. PET data were analyzed using a one-tissue compartment mod

SUBMITTER: Ghazanfari N 

PROVIDER: S-EPMC8905578 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature