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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1993-7-15
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pubmed:abstractText |
Uptake of 7 beta-NBD-NCT ([N-[7-(4-nitrobenzo-2-oxa-1,3-diazol)]-7 beta-amino-3 alpha,12 alpha-dihydroxy-5 beta-cholan-24-oyl)-2'-aminoethanesulfonate) in isolated rat liver hepatocytes occurs by saturable transport without being superimposed by simple diffusion. The dependency of flux rate of uptake on the concentration of 7 beta-NBD-NCT in the presence of Na+ (143 mM) and with Na+ depletion (1 mM) is best described by the assumption of two simple transport systems. Maximal flux rates of uptake Jn and half-saturation constants KT for 7 beta-NBD-NCT are in presence of Na+ for transport system 1 J1(Na+ 143) = 0.15 +/- 0.03 nmol/(min.mg protein) and KT1(Na+ 143) = 3.5 +/- 0.5 microM and for transport system 2 J2(Na+ 143) = 1.0 +/- 0.1 nmol/(min.mg protein) and KT2(Na+ 143) = 190 +/- 25 microM, and in case of Na+ depletion J1(Na+ 1) = 0.1 +/- 0.03 nmol/(min.mg protein), KT1(Na+ 1) = 3.0 +/- 0.5 microM, and J2(Na+ 1) = 0.85 +/- 0.9 nmol/(min.mg protein) and KT2(Na+ 1) = 195 +/- 27 microM. Uptake of 7 beta-NBD-NCT by both transport systems is competitively inhibited by cholyltaurine in the presence of Na+ and with Na+ depletion. Two transport systems are likewise involved in the uptake of cholyltaurine in the presence of Na+ as well as in case of Na+ depletion. Their kinetic parameters are in presence of Na+ J'1(Na+ 143) = 1.55 +/- 0.14 nmol/(min.mg protein) and K'T1(Na+ 143) = 16.1 +/- 3.0 microM, and J'2(Na+ 143) = 0.51 +/- 0.05 nmol/(min.mg protein) and K'T2(Na+ 143) = 38.0 +/- 4.1 microM, and in case of Na+ depletion J'1(Na+ 1) = 0.10 +/- 0.02 nmol/(min.mg protein), K'T1(Na+ 1) = 7.7 +/- 1.2 microM, and J'2(Na+ 1) = 0.40 +/- 0.03 nmol/(min.mg protein) and K'T2(Na+ 1) = 41.0 +/- 4.2 microM. Uptake of cholyltaurine by both transport systems is competitively inhibited by 7 beta-NBD-NCT in the presence of Na+ as well as in case of Na+ depletion. In both cases the inhibition constants are practically identical with the KT values for uptake of 7 beta-NBD-NCT. Photoaffinity labeling of isolated hepatocytes using 7,7-ACT (400 microM) resulted in the irreversible inhibition of uptake of both bile salts to similar extents, confirming the kinetic data that 7 beta-NBD-NCT is a true analogue of cholyltaurine.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/(7,7-azo-3,12-dihydroxy-5-cholan-24-...,
http://linkedlifedata.com/resource/pubmed/chemical/(N-(7-(nitrobenz-2-oxa-1,3-diazol-4-...,
http://linkedlifedata.com/resource/pubmed/chemical/Affinity Labels,
http://linkedlifedata.com/resource/pubmed/chemical/Azo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bile Acids and Salts,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorescent Dyes,
http://linkedlifedata.com/resource/pubmed/chemical/Oxadiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Taurocholic Acid
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2275
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
34
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
741-57
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8509713-Affinity Labels,
pubmed-meshheading:8509713-Animals,
pubmed-meshheading:8509713-Azo Compounds,
pubmed-meshheading:8509713-Bile Acids and Salts,
pubmed-meshheading:8509713-Biological Transport,
pubmed-meshheading:8509713-Diffusion,
pubmed-meshheading:8509713-Fluorescent Dyes,
pubmed-meshheading:8509713-Kinetics,
pubmed-meshheading:8509713-Liver,
pubmed-meshheading:8509713-Male,
pubmed-meshheading:8509713-Microscopy, Fluorescence,
pubmed-meshheading:8509713-Models, Biological,
pubmed-meshheading:8509713-Oxadiazoles,
pubmed-meshheading:8509713-Rats,
pubmed-meshheading:8509713-Rats, Wistar,
pubmed-meshheading:8509713-Taurocholic Acid,
pubmed-meshheading:8509713-Time Factors,
pubmed-meshheading:8509713-Tumor Cells, Cultured
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pubmed:year |
1993
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pubmed:articleTitle |
Fluorescent derivatives of bile salts. III. Uptake of 7 beta-NBD-NCT into isolated hepatocytes by the transport systems for cholyltaurine.
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pubmed:affiliation |
Institut für Organische Chemie und Biochemie, Universität Freiburg, Germany.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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