Abstract:
:The internalization of a neuromodulatory adrenocorticotropic hormone (ACTH) analogue, [125I]ebiratide (H-Met(O2)-Glu[125I]His-Phe-D-Lys-Phe-NH(CH2)2NH2), was examined in cultured monolayers of bovine brain capillary endothelial cells (BCEC). HPLC analysis of the incubation solution showed that [125I]ebiratide was not metabolized during the incubation with BCEC. The acid-resistant binding of [125I]ebiratide to BCEC increased with time for 120 min and showed a significant dependence on temperature and medium osmolarity. Pretreatment of BCEC with dansylcadaverine or phenylarsine oxide, endocytosis inhibitors, and 2,4-dinitrophenol, a metabolic inhibitor, decreased significantly the acid-resistant binding of [125I]ebiratide. The acid-resistant binding of [125I]ebiratide was saturable in the presence of unlabeled ebiratide (100 nM-1 mM). The maximal internalization capacity (Bmax) at 30 min was 7.96 +/- 3.27 pmol/mg of protein with a half-saturation constant (Kd) of 15.9 +/- 6.4 microM. The acid-resistant binding was inhibited by basic peptides such as poly-L-lysine, protamine, histone, and ACTH but was not inhibited by poly-L-glutamic acid, insulin, or transferrin. These results confirmed that ebiratide is transported through the blood-brain barrier via an absorptive-mediated endocytosis.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Terasaki T,Takakuwa S,Saheki A,Moritani S,Shimura T,Tabata S,Tsuji Adoi
10.1023/a:1015848531603subject
Has Abstractpub_date
1992-04-01 00:00:00pages
529-34issue
4eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract:PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910200420
更新日期:1999-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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更新日期:2011-08-01 00:00:00
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更新日期:2001-08-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2011-03-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2006-06-01 00:00:00
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更新日期:2009-07-01 00:00:00
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更新日期:2005-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2003-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2004-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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journal_title:Pharmaceutical research
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更新日期:1984-03-01 00:00:00
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更新日期:2006-03-01 00:00:00
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更新日期:2013-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016226024587
更新日期:1995-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015191511817
更新日期:2002-04-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016218716951
更新日期:1995-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
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更新日期:2016-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0788-3
更新日期:2012-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2016-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026444.67883.83
更新日期:2004-05-01 00:00:00