Measurement of cyclosporin induced changes in P-glycoprotein function at the human blood-brain barrier using [¹⁸F]MC225 and PET.

ABSTRACT:

Introduction

P-glycoprotein (P-gp) or multidrug-resistance protein is one of the most extensively studied efflux transporters at the blood-brain barrier (BBB). Changes in P-gp function are associated with several neurodegenerative and psychiatric diseases, including Alzheimer's disease, Parkinson's disease and schizophrenia and with the bioavailability of several pharmaceuticals in the brain, causing multi-drug resistance or side effects. PET imaging can be used to measure the P-gp function in vivo. This study aims to validate [¹⁸F]MC225 as specific P-gp PET tracer with the use of cyclosporin as selective P-gp inhibitor.

Methods

Fourteen healthy volunteers (age 67 ± 5y) were included. Subjects underwent twice a 60 min dynamic [¹⁸F]MC225 (200MBq) PET sca

SUBMITTER: Mossel P 

PROVIDER: S-EPMC12491356 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature