[¹¹C]metoclopramide is a sensitive radiotracer to measure moderate decreases in P-glycoprotein function at the blood-brain barrier.

ABSTRACT: The efflux transporter P-glycoprotein (P-gp) at the blood-brain barrier limits the cerebral uptake of various xenobiotics. To assess the sensitivity of [¹¹C]metoclopramide to measure decreased cerebral P-gp function, we performed [¹¹C]metoclopramide PET scans without (baseline) and with partial P-gp inhibition by tariquidar in wild-type, heterozygous Abcb1a/b^(+/-) and homozygous Abcb1a/b^(-/-) mice as models with controlled levels of cerebral P-gp expression. Brains were collected to quantify P-gp expression with immunohistochemistry. Brain uptake of [¹¹C]metoclopramide was expressed as the area under the brain time-activity curve (AUC_brain) and compared with data previously obtained with (R)-[¹¹

SUBMITTER: Mairinger S 

PROVIDER: S-EPMC10905639 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature