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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
|
| pubmed:dateCreated |
1997-1-30
|
| pubmed:abstractText |
Adenosine receptor signal transduction mechanisms have previously been characterized in Syrian hamster smooth muscle DDT1 MF-2 cells but adenosine transport in these cells has not. DDT1 MF-2 cells possess a high density (370,000 sites/cell) of high affinity (Kd value of 0.26 nM) binding sites for [3H]nitrobenzylthioinosine, a marker for the equilibrative and inhibitor-sensitive subtype of nucleoside transporters. Transport of [3H]adenosine was insensitive to Na+ and was inhibited by the nucleoside transport inhibitors nitrobenzylthioinosine, dilazep and dipyridamole with IC50 values of 1, 13 and 270 nM, respectively. Propentofylline, a neuroprotective compound that can inhibit nucleoside transporters, is rapidly metabolized in vivo to the racemate (+/-)-A720287. Based on recent findings that some transport inhibitors exhibit marked stereoselectivity, we tested the degree to which individual stereoisomers of (+/-)-A720287 affect adenosine transport. Propentofylline inhibited [3H]adenosine transport in DDT1 MF-2 cells with an IC50 value of 24 microM. (+/-)-A720287 and the individual stereoisomers (+)-833791 and (-)-844261 had similar potency to propentofylline for inhibition of [3H]adenosine transport in DDT1 MF-2 cells as well as in clonal mouse leukemia L1210/B23.1 cells, cells which possess only the equilibrative and inhibitor-sensitive subtype of nucleoside transporters. Thus, the neuroprotective effects of propentofylline may be due, in part, to the primary metabolites of propentofylline.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/4-nitrobenzylthioinosine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/Dilazep,
http://linkedlifedata.com/resource/pubmed/chemical/Dipyridamole,
http://linkedlifedata.com/resource/pubmed/chemical/Thioinosine,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthines,
http://linkedlifedata.com/resource/pubmed/chemical/propentofylline
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jul
|
| pubmed:issn |
0014-2999
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
11
|
| pubmed:volume |
308
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
97-102
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:8836637-Adenosine,
pubmed-meshheading:8836637-Animals,
pubmed-meshheading:8836637-Binding Sites,
pubmed-meshheading:8836637-Biological Transport,
pubmed-meshheading:8836637-Cricetinae,
pubmed-meshheading:8836637-Dilazep,
pubmed-meshheading:8836637-Dipyridamole,
pubmed-meshheading:8836637-Genital Neoplasms, Male,
pubmed-meshheading:8836637-Kinetics,
pubmed-meshheading:8836637-Leiomyosarcoma,
pubmed-meshheading:8836637-Leukemia L1210,
pubmed-meshheading:8836637-Male,
pubmed-meshheading:8836637-Mesocricetus,
pubmed-meshheading:8836637-Muscle, Smooth,
pubmed-meshheading:8836637-Rats,
pubmed-meshheading:8836637-Thioinosine,
pubmed-meshheading:8836637-Tumor Cells, Cultured,
pubmed-meshheading:8836637-Vas Deferens,
pubmed-meshheading:8836637-Xanthines
|
| pubmed:year |
1996
|
| pubmed:articleTitle |
[3H]adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline.
|
| pubmed:affiliation |
Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg, Canada.
|
| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|