Peptide Carrier-Mediated Transport in Intestinal Brush Border Membrane Vesicles of Rats and Rabbits: Cephradine Uptake and Inhibition
dc.contributor.author | Fleisher, David | en_US |
dc.contributor.author | Yuasa, Hiroaki | en_US |
dc.contributor.author | Amidon, Gordon L. | en_US |
dc.date.accessioned | 2006-09-08T19:14:58Z | |
dc.date.available | 2006-09-08T19:14:58Z | |
dc.date.issued | 1993-03 | en_US |
dc.identifier.citation | Yuasa, Hiroaki; Amidon, Gordon L.; Fleisher, David; (1993). "Peptide Carrier-Mediated Transport in Intestinal Brush Border Membrane Vesicles of Rats and Rabbits: Cephradine Uptake and Inhibition." Pharmaceutical Research 10(3): 400-404. <http://hdl.handle.net/2027.42/41430> | en_US |
dc.identifier.issn | 1573-904X | en_US |
dc.identifier.issn | 0724-8741 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/41430 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=8464813&dopt=citation | en_US |
dc.description.abstract | The uptake kinetics of cephradine, an amino-β-lactam antibiotic, were studied in rat and rabbit intestinal brush border membrane vesicles preparations using both the Ca 2+ and the Mg 2+ methods of preparation, in the presence of an inward proton gradient. The Ca 2+ method demonstrated greater uptake of cephradine in intestinal brush border vesicles prepared from both rat and rabbit and was used for these studies. The transport was observed to be of Michaelis–Menten carrier-mediated type with a passive transport component. The kinetic parameters obtained were as follows: for rat and rabbit, respectively, K m , 1.6 and 1.9 m M ; J max ′, 1.7 and 20.7 nmol/mg/min; P c ′ (= J max ′/ K m ), 1.1 and 10.9 µL/mg/min; and P m ′, 0.4 and 0.8 µL/mg/min. The kinetic parameters for the rat vesicles are consistent with those from our previous perfusion study using a conversion factor of 0.71 cm 2 /mg protein. The rabbit vesicles exhibited a similar Michaelis constant and a 10-fold larger maximal transport velocity, suggesting a quantitative advantage for the study of carrier-mediated transport in the rabbit compared to rat vesicles from the intestine. Cephradine uptake was inhibited by phenylpropionylproline, a proline derivative, and enalapril, an ACE inhibitor, which do not have an α-amino group, as well as dipeptides, tripeptides, and amino-β-lactam antibiotics in both rat and rabbit vesicles. These results support the suggestion that they share the same peptide carrier pathway for oral absorption and that the vesicles may be a useful tool in developing orally effective peptide-type drugs. | en_US |
dc.format.extent | 1038120 bytes | |
dc.format.extent | 3115 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Kluwer Academic Publishers-Plenum Publishers; Plenum Publishing Corporation ; Springer Science+Business Media | en_US |
dc.subject.other | Rabbit | en_US |
dc.subject.other | Rat | en_US |
dc.subject.other | Tripeptides | en_US |
dc.subject.other | Proline Derivatives | en_US |
dc.subject.other | Dipeptides | en_US |
dc.subject.other | Peptide Carrier | en_US |
dc.subject.other | Intestinal Uptake | en_US |
dc.subject.other | Cephradine | en_US |
dc.subject.other | ACE Inhibitors | en_US |
dc.subject.other | Amino β-Lactam Antibiotics | en_US |
dc.subject.other | Medical Law | en_US |
dc.subject.other | Biomedicine | en_US |
dc.subject.other | Brush Border Membrane Vesicles | en_US |
dc.subject.other | Pharmacy | en_US |
dc.subject.other | Pharmacology/Toxicology | en_US |
dc.subject.other | Biochemistry, General | en_US |
dc.subject.other | Biomedical Engineering | en_US |
dc.title | Peptide Carrier-Mediated Transport in Intestinal Brush Border Membrane Vesicles of Rats and Rabbits: Cephradine Uptake and Inhibition | en_US |
dc.type | Article | en_US |
dc.subject.hlbsecondlevel | Pharmacy and Pharmacology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan, 48109-1065 | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan, 48109-1065 | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Michigan, 48109-1065 | en_US |
dc.contributor.affiliationumcampus | Ann Arbor | en_US |
dc.identifier.pmid | 8464813 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/41430/1/11095_2004_Article_304789.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1023/A:1018940306394 | en_US |
dc.identifier.source | Pharmaceutical Research | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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