Abstract:
PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RESULTS:Cereport increased the HBMEC permeability to [14C]-inulin, but not to [3H]-dextran. The effect was transient, maximal at 15 min (i.e., 79.3% increase), and polarized to the basolateral membrane. An inverted U, dose-response curve was observed with active concentrations of Cereport from 0.01 to 0.5 nmol/L, the plateau maximal effect between 0.5 and 10 nmol/L, and loss of activity at the highest concentration, i.e., 20 nmol/L. Cyclic AMP-specific phosphodiesterase 3 (PDE3) inhibitor rolipram (10 micromol/L) abolished Cereport effects, while cGMP-specific PDE5 inhibitor, zaniprast (50 micromol/L) enhanced by 31% (p < 0.05) the effect of 0.1 nmolL Cereport. Unlabeled Cereport displaced [125I]-bradykinin and/or [125I]-Cereport from the basolateral side. There was no specific Cereport binding to the apical side. CONCLUSIONS:Cereport exerts specific time, dose and size dependent actions on HMBEC monolayer that are restricted to the basolateral membrane. Its effects can be further modulated through changes in cAMP and cGMP second messenger systems.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BVdoi
10.1023/a:1018938722768subject
Has Abstractpub_date
1999-09-01 00:00:00pages
1360-5issue
9eissn
0724-8741issn
1573-904Xjournal_volume
16pub_type
杂志文章abstract:PURPOSE:Evista (raloxifene HCl) is a nonsteroidal selective estrogen receptor modulator that displays estrogen agonist effects on bone and lipid metabolism but estrogen antagonist effects on the breast and endometrium. The potential for drug-drug interaction between raloxifene and warfarin was assessed in 15 healthy po...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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doi:10.1023/a:1011033326980
更新日期:2001-05-01 00:00:00
abstract::The effect of different concentrations of polyvinyl alcohol 14000 and 72000 (PVA 14 and 72) on the activity of betamethasone and phenylephrine hydrochloride in the rabbit eye was investigated. The polymer of higher molecular weight exerts a more pronounced effect at relatively lower viscosities. Effects on the intraoc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016398915965
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abstract::Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018967401000
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abstract::Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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journal_title:Pharmaceutical research
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doi:10.1007/s11095-006-9204-1
更新日期:2007-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015811830830
更新日期:1991-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018964401677
更新日期:1993-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2332-y
更新日期:2018-02-21 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1368-5
更新日期:2014-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011907201096
更新日期:1998-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0695-7
更新日期:2012-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016243706415
更新日期:1995-10-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...
journal_title:Pharmaceutical research
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更新日期:2019-07-31 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1020492213172
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2085-z
更新日期:2017-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1139-8
更新日期:2013-09-01 00:00:00
abstract::The physicochemical properties and crystal structures of the crystalline salts formed by the interaction of an achiral anion, salicylate, with homochiral and racemic ephedrinium and pseudoephedrinium cations were determined. The interaction of ephedrinium or pseudoephedrinium with salicylate in aqueous solution yielde...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018945401484
更新日期:1994-11-01 00:00:00
abstract::Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015888813741
更新日期:1992-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2428-z
更新日期:2018-05-22 00:00:00
abstract:PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1579-9
更新日期:2015-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1361-z
更新日期:2014-10-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1154-9
更新日期:2014-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026470831256
更新日期:2000-10-01 00:00:00
abstract::The transient dynamic swelling and dissolution behavior during the release of a growth hormone releasing peptide, [D-Trp2-D-Phe5]GHRP, from erodible, non-cross-linked poly(methyl methacrylate-co-methacrylic acid) (PMMA/MAA) beads has been investigated at pH 7.4 as a function of buffer concentration. Although the swell...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018902404036
更新日期:1993-07-01 00:00:00