Memantine transport by a proton-coupled organic cation antiporter in hCMEC/D3 cells, an in vitro human blood-brain barrier model

• Published in: Drug metabolism and pharmacokinetics Vol. 30; no. 2; pp. 182 - 187
• Main Authors: Higuchi, Kei, Kitamura, Atsushi, Okura, Takashi, Deguchi, Yoshiharu
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.04.2015
• Subjects: Active transport; Biological Transport; Blood-Brain Barrier - cytology; Blood-Brain Barrier - drug effects; Blood-Brain Barrier - metabolism; Blood–brain barrier; Cell Line, Transformed; Endothelial Cells - drug effects; Endothelial Cells - metabolism; Feasibility Studies; hCMEC/D3 cells; Humans; Kinetics; Memantine; Memantine - metabolism; Membrane Transport Modulators - pharmacology; Models, Biological; Organic Cation Transport Proteins - antagonists & inhibitors; Organic Cation Transport Proteins - metabolism; Proton-coupled organic cation antiporter; RNA Interference; Transfection; Proton-coupled organic cation antiporter; Active transport; Memantine; hCMEC/D3 cells; Blood–brain barrier

Memantine is clinically used for the treatment of patients with Alzheimer's disease and is highly distributed to the brain. The aim of this study is to characterize memantine transport at the blood–brain barrier (BBB) using hCMEC/D3 cells, a human BBB model. The initial uptake velocity of meman...