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Drug transport across the blood-brain barrier
It is expected that improved knowledge of the anatomical and physiological aspects of the blood-brain barrier and its regulation will provide a scientific basis for the development of strategies to improve the transport of drugs into the central nervous system. Expand
Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier.
It is shown that the lack of Mrp1 protein causes etoposide levels to increase about 10-fold in the CSF after intravenous administration of the drug. Expand
The influence of cytokines on the integrity of the blood-brain barrier in vitro
In conclusion, cytokines induce a disruption of the BBB in vitro and cyclooxygenase activation within the endothelial cells seems to play a key role. Expand
Lamotrigine, a new anticonvulsant: Pharmacokinetics in normal humans
The pharmacokinetics of lamotrigine, a new anticonvulsant, were studied in three studies in normal volunteers, suggesting the absence of autoinduction of metabolism. Expand
Penetration of dexamethasone into brain glucocorticoid targets is enhanced in mdr1A P-glycoprotein knockout mice.
It was found that brain areas expressing the glucocorticoid receptor in high abundance, such as the hippocampal cell fields and the paraventricular nucleus, showed a 10-fold increase in cell nuclear uptake of radiolabeled steroid, which supports the concept of a pituitary site of action of dexamethasone in blockade of stress-induced ACTH release. Expand
The blood-brain barrier in neuroinflammatory diseases.
The existence of the blood-brain barrier (BBB)bwas revealed through studies by [Ehrlich (1885)][1] in the late 19th century, describing that brain tissue remained unstained after injection of a vitalExpand
Establishment and functional characterization of an in vitro model of the blood-brain barrier, comprising a co-culture of brain capillary endothelial cells and astrocytes.
A high quality and mass-production in vitro BBB model was established in which experiments with physiological, pharmacological and pathophysiological objectives can be reproducibly performed. Expand
Methodological considerations of intracerebral microdialysis in pharmacokinetic studies on drug transport across the blood–brain barrier
Several microdialysis studies on BBB transport of drugs are presented showing that intracerebral micro dialysis is capable to assess localBBB transport profiles and methods have been proposed to determine recovery values. Expand
Methodological issues in microdialysis sampling for pharmacokinetic studies.
With the progress of analytical methodology, especially with respect to low volume/low concentration measurements and simultaneous measurement of multiple compounds, the applications and importance of the microdialysis technique in pharmacokinetic research will continue to increase. Expand
Pharmacokinetic‐pharmacodynamic modeling of the central nervous system effects of midazolam and its main metabolite α‐hydroxymidazolam in healthy volunteers
It seems that α‐hydroxymidazolam is highly potent with respect to the measured effects and contributes significantly to those effects of midazol am after oral administration. Expand