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In vitro and in vivo studies on the metabolism of tirofiban

Autor: S, Vickers, A D, Theoharides, B, Arison, S K, Balani, D, Cui, C A, Duncan, J D, Ellis, L M, Gorham, S L, Polsky, T, Prueksaritanont, H G, Ramjit, D E, Slaughter, K P, Vyas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 27(11)

Tirofiban hydrochloride [L-tyrosine-N-(butylsulfonyl)-O-[4-(4-piperidinebutyl)] monohydrochloride, is a potent and specific fibrinogen receptor antagonist. Radiolabeled tirofiban was synthesized with either (3)H-label incorporated into the phenyl rin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::4696503da3064ea7bc781db54227d249
https://pubmed.ncbi.nlm.nih.gov/10534322

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In vitro and in vivo evaluations of intestinal barriers for the zwitterion L-767,679 and its carboxyl ester prodrug L-775,318. Roles of efflux and metabolism

Autor: T, Prueksaritanont, P, DeLuna, L M, Gorham, B, Ma, D, Cohn, J, Pang, X, Xu, K, Leung, J H, Lin

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 26(6)

The barriers to oral delivery of the hydrophilic zwitterion L-767, 679 (I) and its carboxyl ester prodrug L-775,318 (II) were examined. In the Caco-2 cell model, transport of II, but not I, was strongly oriented in the secretory direction. The basal-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::9ff44de5bb0bf76ca059015360c313fe
https://pubmed.ncbi.nlm.nih.gov/9616186

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In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s

Autor: T, Prueksaritanont, L M, Gorham, B, Ma, L, Liu, X, Yu, J J, Zhao, D E, Slaughter, B H, Arison, K P, Vyas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 25(10)

Simvastatin (SV) is a lactone prodrug used for the treatment of hypercholesterolemia. Upon incubation of SV with liver microsomal preparations from human donors, four major metabolic products were formed (3'-hydroxy SV, 6'-exomethylene SV, 3',5'-dihy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::85fdf62fc5a637a26621c6499d69e9cd
https://pubmed.ncbi.nlm.nih.gov/9321523

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In vitro and in vivo evaluations of the metabolism, pharmacokinetics, and bioavailability of ester prodrugs of L-767,679, a potent fibrinogen receptor antagonist: an approach for the selection of a prodrug candidate

Autor: T, Prueksaritanont, L M, Gorham, M J, Breslin, J H, Hutchinson, G D, Hartman, K P, Vyas, T A, Baillie

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 25(8)

The present study demonstrates the utility of an in vitro-in vivo correlative approach in the selection of an optimum prodrug candidate of L-767,679 (N-([7-(piperazin-1-yl)-3,4-dihydro-1(1H)-isoquinolinone-2-yl]acetyl)-3(S)-(ethynyl)-beta-alanine), a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f498549b2c4a50b0c5276eef59ac263d
https://pubmed.ncbi.nlm.nih.gov/9280406

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Disposition of L-738,167, a potent and long-acting fibrinogen receptor antagonist, in dogs. Dose-dependent pharmacokinetics

Autor: T, Prueksaritanont, L M, Gorham, J A, Naue, T G, Hamill, B C, Askew, K P, Vyas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 25(3)

L-738,167 is a potent and long-acting fibrinogen receptor antagonist and may be useful for treatment of chronic thrombotic occlusive disorders. The purposes of this study were to characterize the metabolism and disposition of L-738,167, and to invest

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::11d26179278dc05f31096da0da275982
https://pubmed.ncbi.nlm.nih.gov/9172954

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Species and organ differences in first-pass metabolism of the ester prodrug L-751,164 in dogs and monkeys. In vivo and in vitro studies

Autor: T, Prueksaritanont, L M, Gorham, J D, Ellis, C, Fernandez-Metzler, P, Deluna, J R, Gehret, K L, Strong, J H, Hochman, B C, Askew, M E, Duggan, J D, Gilbert, J H, Lin, K P, Vyas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 24(11)

The pharmacokinetics and bioavailability of L-751,164, an ethyl ester prodrug of a potent fibrinogen receptor antagonist, L-742,998, were studied in beagle dogs and rhesus monkeys. In both species, L-751,164 exhibited high clearance. After an intrave

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7a21deb0676661bffbaf88aad293d60d
https://pubmed.ncbi.nlm.nih.gov/8937862

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Comparative studies of drug-metabolizing enzymes in dog, monkey, and human small intestines, and in Caco-2 cells

Autor: T, Prueksaritanont, L M, Gorham, J H, Hochman, L O, Tran, K P, Vyas

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 24(6)

Drug-metabolizing enzymes were studied in subcellular fractions of dog, monkey, and human small intestines, and in the human adenocarcinoma cell line Caco-2, a commonly used in vitro absorption model. Immunoblot analysis indicated the presence of enz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::efc1428a2d33c07df26c786eff9040fa
https://pubmed.ncbi.nlm.nih.gov/8781778

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