Document Detail


Saturation kinetics, specificity and NBMPR sensitivity of thymidine entry into the central nervous system.
MedLine Citation:
PMID:  9237518     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
It was not until the development of a technique that could measure the brain uptake of slowly moving substrates, that the saturable transport system at the blood-brain barrier (BBB) for the pyrimidine deoxyribonucleoside, thymidine, was demonstrated. The aim of this present study was to further characterize this saturable uptake system at the blood-brain and blood-CSF barriers in terms of specificity, 6-(4-nitrobenzyl)thio-9-beta-D-ribofuranosylpurine (NBMPR) sensitivity and saturation kinetics by means of the in situ brain perfusion technique in anaesthetized guinea pigs. The results indicated that the transport system identified for [3H]thymidine can also transport other pyrimidine deoxyribonucleosides (deoxycytidine) and pyrimidine ribonucleosides (uridine) and is partially NBMPR-sensitive. In addition, guanosine, monocarboxylic acids, hexoses or amino acids were not substrates for the transport system. Further studies revealed that the transport system for [3H]thymidine at the BBB has a low affinity (Km 0.20 +/- 0.06 mM), but a relatively high capacity (Vmax 1.06 +/- 0.08 nmol min(-1) g(-1)). Overall, this study is indicative of a NBMPR-sensitive (es) facilitative transport system for [3H]thymidine and the likely presence of a NBMPR-insensitive and/or sodium-dependent transport system of the N2 (cit) type at the blood-brain and blood-CSF barriers of the guinea pig.
Authors:
S A Thomas; M B Segal
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Brain research     Volume:  760     ISSN:  0006-8993     ISO Abbreviation:  Brain Res.     Publication Date:  1997 Jun 
Date Detail:
Created Date:  1997-10-28     Completed Date:  1997-10-28     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0045503     Medline TA:  Brain Res     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  59-67     Citation Subset:  IM    
Affiliation:
Sherrington School of Physiology, UMDS St. Thomas' Hospital Campus, University of London, UK. sarah.thomas@umds.ac.uk
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MeSH Terms
Descriptor/Qualifier:
Affinity Labels / pharmacology*
Animals
Biological Transport / physiology
Central Nervous System / drug effects,  metabolism*
Dose-Response Relationship, Drug
Guinea Pigs
Kinetics
Sensitivity and Specificity*
Thioinosine / analogs & derivatives*,  pharmacology
Thymidine / pharmacokinetics*
Chemical
Reg. No./Substance:
0/Affinity Labels; 38048-32-7/4-nitrobenzylthioinosine; 50-89-5/Thymidine; 574-25-4/Thioinosine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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