title: Tissue plasminogen activator inhibits P-glycoprotein activity in brain endothelial cells.
abstract: Tissue plasminogen activator (0.01-30 microgram/ml) dose-dependently inhibited the functional activity of P-glycoprotein, assessed by rhodamine 123 accumulation in GP8 immortalized rat brain endothelial cells, but this effect was unrelated to its proteolytic activity. Elevation of intra-endothelial cyclic AMP concentration and stimulation of protein kinase C increased P-glycoprotein activity in GP8 cells and also attenuated the tissue plasminogen activator-induced inhibition.
authors.affiliation: Department of Pharmacology 1, Nagasaki University School of Medicine, 1-12-4 Sakamoto, 852-8523, Nagasaki, Japan. deli-ngs@umin.ac.jp
authors.forename: M A
authors.initials: MA
authors.lastname: Deli
authors.forename: C S
authors.initials: CS
authors.lastname: Abrahám
authors.forename: H
authors.initials: H
authors.lastname: Takahata
authors.forename: M
authors.initials: M
authors.lastname: Niwa
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D001812:Blood-Brain Barrier; D001921:Brain / Q000166:cytology / Q000378:metabolism; D002461:Cell Line, Transformed; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D020112:Rhodamine 123 / Q000378:metabolism; D010959:Tissue Plasminogen Activator / Q000494:pharmacology*
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D020112:Rhodamine 123; D010959:Tissue Plasminogen Activator