Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1997-8-7
pubmed:abstractText
The transport of a fluorescent rapamycin derivative was measured in killifish (Fundulus heteroclitus) renal proximal tubules by means of confocal microscopy and image analysis. Renal cells and tubular lumens rapidly accumulated the rapamycin analog from the medium and attained steady state within 60 min. At steady state, luminal fluorescence intensity was two to four times higher than cellular fluorescence. Cellular fluorescence intensity was a linear function of medium substrate concentration and was not affected by any treatment used. In contrast, luminal fluorescence exhibited a saturable component as the medium concentration of the rapamycin derivative was increased. Secretion into the lumen was blocked by KCN, rapamycin, cyclosporin A and substrates for p-glycoprotein (verapamil, PSC-833 and FK506), but not by substrates for the renal organic anion or organic cation transport systems, such as p-aminohippurate, leukotriene C4 or tetraethylammonium. Finally, rapamycin blocked p-glycoprotein-mediated secretion of a fluorescent cyclosporin A derivative. The data are consistent with the fluorescent rapamycin analog entering proximal tubule cells by simple diffusion and then being pumped into the tubular lumen by p-glycoprotein. They suggest that the parent compound, rapamycin, would be handled similarly.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
282
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
440-4
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
p-Glycoprotein-mediated transport of a fluorescent rapamycin derivative in renal proximal tubule.
pubmed:affiliation
Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't