Zobrazeno 1 - 10 of 120 pro vyhledávání: '"R T, Borchardt"'
1
An efficient in vitro assay for acetylcholinesterase reactivators using immobilized enzyme
Autor: A M, Trammel, J E, Simmons, R T, Borchardt
Publikováno v: Pharmaceutical research. 1(3)
A new and efficient in vitro assay for evaluating reactivators of organophosphate-inhibited acetylcholinesterase has been developed. Low density polyethylene beads (4 mm) were func-tionalized to terminal aldehydes and used to immobilize acetylcholine
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::177d9f3e6e227e516bb9737a40ca0804
https://pubmed.ncbi.nlm.nih.gov/24277247
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2
Characterization of an in vitro blood-brain barrier model system for studying drug transport and metabolism
Autor: K L, Audus, R T, Borchardt
Publikováno v: Pharmaceutical research. 3(2)
Bovine brain micro vessel endothelial cells have been isolated and grown in culture to monolayers. These endothelial cell monolayers have been characterized morphologically with electron microscopy, histochemically for brain endothelium enzyme marker
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3dd457ad51703576c15dfdeded472575
https://pubmed.ncbi.nlm.nih.gov/24271465
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3
In vitro drug absorption models. I. Brush border membrane vesicles, isolated mucosal cells and everted intestinal rings: characterization and salicylate accumulation
Autor: I, Osiecka, P A, Porter, R T, Borchardt, J A, Fix, C R, Gardner
Publikováno v: Pharmaceutical research. 2(6)
Brush border membrane vesicles, isolated mucosal cells and everted rings from rat intestine were compared for their suitability for drug uptake studies. Vesicles from brush border membranes were judged to be metabolically and morphologically function
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ff52ad943b7f41e91d4acc7240994a65
https://pubmed.ncbi.nlm.nih.gov/24271125
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4
Hidalgo, I. J., Raub, T. J., and Borchardt, R. T.: Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability, Gastroenterology, 96, 736-749, 1989--the backstory
Autor: I J, Hidalgo, T J, Raub, R T, Borchardt
Publikováno v: The AAPS journal. 13(3)
Caco-2 cells develop morphologic characteristics of normal enterocytes when grown on plastic dishes or nitrocellulose filters. The purpose of this study was to determine whether Caco-2 cells undergo similar differentiation when grown on Transwell pol
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab77905cf30a49cd6ed11a79dbca6108
https://pubmed.ncbi.nlm.nih.gov/2914637
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5
Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using a 3-(2'-hydroxy-4',6'-dimethylphenyl)-3,3-dimethyl propionic Acid promoiety
Autor: B, Wang, S, Gangwar, G, Pauletti, T, Siahaan, R T, Borchardt
Publikováno v: Methods in molecular medicine. 23
One of the major obstacles to the development of biologically active peptides as clinically useful therapeutic agents has been their low permeation through biological barriers (e.g., intestinal mucosa, blood-brain barrier) and their metabolic labilit
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ae2e2c1dd31eca445765a0600129a783
https://pubmed.ncbi.nlm.nih.gov/21380891
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6
Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using an acyloxyalkoxy promoiety
Autor: S, Gangwar, G M, Pauletti, T J, Siahaan, V J, Stella, R T, Borchardt
Publikováno v: Methods in molecular medicine. 23
The clinical development of orally active peptide drugs has been limited by their unfavorable physicochemical characteristics (e.g., charge, hydrogen bonding potential, size), which prevent them from permeating biological barriers such as the intesti
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a0a0e01ed31930e8a7f0fa84fc7368b7
https://pubmed.ncbi.nlm.nih.gov/21380890
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7
Synthesis of coumarin-based, esterase-sensitive cyclic prodrugs of opioid peptides with enhanced membrane permeability and enzymatic stability
Autor: B, Wang, D, Shan, W, Wang, H, Zhang, O, Gudmundsson, R T, Borchardt
Publikováno v: Methods in molecular medicine. 23
With the discovery of an increasing number of biologically active peptides and peptide mimetics (1-3), there is a pressing need for the development of strategies to deliver these biologically active compounds to the desired site of action. The preced
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e7d5e829cb7c06237438d0b8016980fe
https://pubmed.ncbi.nlm.nih.gov/21380892
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10
Synthesis and conformational analysis of a coumarinic acid-based cyclic prodrug of an opioid peptide with modified sensitivity to esterase-catalyzed bioconversion
Autor: H, Ouyang, D G, Vander Velde, R T, Borchardt, T J, Siahaan
Publikováno v: The journal of peptide research : official journal of the American Peptide Society. 59(4)
The coumarinic acid-based cyclic DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH) prodrug 1a exhibited more favorable physicochemical properties than did DADLE for permeation across the intestinal mucosa. However, prodrug 1a, whose bioconversion to DADLE was slo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f0a129dd40dd6e49c306988b711e82e5
https://pubmed.ncbi.nlm.nih.gov/11972752
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