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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
1987-7-1
pubmed:abstractText
The affinities of adenosine and 2-chloroadenosine for the nucleoside transport system of guinea pig myocytes were evaluated indirectly by studying the inhibition of the binding of [3H]nitrobenzylthioinosine and directly by measuring the influx of [3H]radiolabeled substrates. Maximal transport velocities of the two nucleosides were also obtained. [3H]Nitrobenzylthioinosine bound to a single class of high-affinity sites (KD of 0.8 nM) which possessed a maximal binding capacity (Bmax) of 870,000 sites/cell. Adenosine, 2-chloroadenosine or the nucleoside transport inhibitor, dipyridamole, competitively inhibited the site-specific binding of [3H]nitrobenzylthioinosine with Ki values of 318 microM, 22 microM and 75 nM respectively. Both [3H]adenosine and [3H]2-chloroadenosine entered myocytes in a saturable and inhibitible manner. Observed transport kinetic constants (Km and Vmax) were 146 microM and 24.2 pmoles/10(6) cells/sec, respectively, for adenosine and 36 microM and 11.7 pmoles/10(6) cells/sec, respectively for 2-chloroadenosine. Affinities of adenosine, 2-chloroadenosine, nitrobenzylthioinosine and dipyridamole for the nucleoside transport system derived from binding and influx methodologies were equivalent which confirms that [3H]nitrobenzylthioinosine binding sites are closely associated with the nucleoside transporter.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1275-80
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Nucleoside transport in guinea pig myocytes. Comparison of the affinities and transport velocities for adenosine and 2-chloroadenosine.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't