ISSN:
1573-904X
Schlagwort(e):
H1-antagonist
;
blood-brain barrier (BBB)
;
propranolol
;
lipophilic basic drugs
;
common transport system
Quelle:
Springer Online Journal Archives 1860-2000
Thema:
Chemie und Pharmazie
Notizen:
Abstract The blood-brain barrier (BBB) transport system for H1 antagonists was studied using primary cultured bovine brain capillary endothelial cells (BCEC). The uptake of [3H]mepyramine was inhibited by various H1-antagonists. Ketotifen competitively inhibited [3H]mepyramine uptake with an inhibition constant (Ki ) of 46.8 µM. Lipophilic basic drugs such as propranolol, lidocaine and imipramine significantly inhibited [3H]mepyramine uptake. In particular, propranolol inhibited [3H]mepyramine uptake competitively at an inhibition constant (Ki) of 51.1 µM. Moreover, in ATP-depleted BCEC, [3H]mepyramine uptake was stimulated by preloading with H1- antagonists and lipophilic basic drugs. These results indicated that H1-antagonists are transported across the BBB via a carrier-mediated transport system common to lipophilic basic drugs.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1023/A:1018980914687
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