Abstract
The transport mechanism of the H1antagonist mepyramine at the blood-brain barrier (BBB) was studied by using primary cultured monolayers of bovine brain capillary endothelial cells (BCEC). The initial uptake of [3H]mepyramine into the BCEC showed strong temperature and concentration dependency, indicating that it involves both saturable and nonsaturable processes. Transport at the luminal membrane may be the rate-limiting process in the transcellular transport, since the values of the uptake coefficient of [3H]mepyramine at the luminal membrane (609 µl/mg protein/min) and the transcellular permeability coefficient (488 µl/mg protein/min) are very similar. The initial uptake of [3H]mepyramine was not affected by metabolic inhibitors, but was stimulated by preloading with the drug. Mepyramine appears to be transported into the BCEC by a carrier-mediated transport system which does not require metabolic energy, probably via a facilitated diffusion mechanism.
Original language | English |
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Pages (from-to) | 975-978 |
Number of pages | 4 |
Journal | Pharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists |
Volume | 11 |
Issue number | 7 |
DOIs | |
Publication status | Published - 1994 Jul |
Keywords
- H-antagonist
- blood-brain barrier transport
- carrier-mediated transport
- mepyramine
- primary cultured brain capillary endothelial cells
ASJC Scopus subject areas
- Biotechnology
- Molecular Medicine
- Pharmacology
- Pharmaceutical Science
- Organic Chemistry
- Pharmacology (medical)