Carrier-mediated transport of baclofen across monolayers of bovine brain endothelial cells in primary culture.
The mechanism of transport of baclofen, a centrally acting muscle relaxant, across the blood-brain barrier (BBB) was studied using an in vitro model. The model consisted of a monolayer of bovine brain endothelial cells grown in primary culture on a porous regenerated cellulose membrane. The transport of baclofen across the monolayer expressed time and concentration dependency and was saturable. Transport data were corrected for diffusion and fitted to the Michaelis-Menten Vmax model: Km = 58.5 microM, Vmax = 0.23 nmol/min. The results validate the use of the in vitro BBB model as described and support the hypothesis that baclofen penetrates the BBB by means of a carrier-mediated transport system.
van Bree
J B
JB
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence 66045.
Audus
K L
KL
Borchardt
R T
RT
D000818:Animals; D001418:Baclofen / Q000378:metabolism*; D001693:Biological Transport, Active; D001812:Blood-Brain Barrier; D001921:Brain / Q000166:cytology / Q000378:metabolism*; D002417:Cattle; D002478:Cells, Cultured; D004727:Endothelium / Q000166:cytology / Q000378:metabolism; D008833:Microcirculation; D008954:Models, Biological; D013696:Temperature
D001418:Baclofen