[3H]adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline.
Identifieur interne : 004342 ( Main/Merge ); précédent : 004341; suivant : 004343[3H]adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline.
Auteurs : F E Parkinson [Canada] ; K. Mukherjee ; J D GeigerSource :
- European journal of pharmacology [ 0014-2999 ] ; 1996.
English descriptors
- KwdEn :
- Adenosine (metabolism), Animals, Binding Sites, Biological Transport (drug effects), Cricetinae, Dilazep (pharmacology), Dipyridamole (pharmacology), Genital Neoplasms, Male (metabolism), Kinetics, Leiomyosarcoma (metabolism), Leukemia L1210 (metabolism), Male, Mesocricetus, Muscle, Smooth (drug effects), Muscle, Smooth (metabolism), Rats, Thioinosine (analogs & derivatives), Thioinosine (metabolism), Thioinosine (pharmacology), Tumor Cells, Cultured, Vas Deferens (drug effects), Vas Deferens (metabolism), Xanthines (metabolism), Xanthines (pharmacology).
- MESH :
- chemical , analogs & derivatives : Thioinosine.
- chemical , metabolism : Adenosine, Thioinosine, Xanthines.
- drug effects : Biological Transport, Muscle, Smooth, Vas Deferens.
- metabolism : Genital Neoplasms, Male, Leiomyosarcoma, Leukemia L1210, Muscle, Smooth, Vas Deferens.
- chemical , pharmacology : Dilazep, Dipyridamole, Thioinosine, Xanthines.
- Animals, Binding Sites, Cricetinae, Kinetics, Male, Mesocricetus, Rats, Tumor Cells, Cultured.
Abstract
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: 8836637
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">[3H]adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline.</title><author><name sortKey="Parkinson, F E" sort="Parkinson, F E" uniqKey="Parkinson F" first="F E" last="Parkinson">F E Parkinson</name><affiliation wicri:level="4"><nlm:affiliation>Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg, Canada.</nlm:affiliation><country xml:lang="fr">Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg</wicri:regionArea><orgName type="university">Université du Manitoba</orgName><placeName><settlement type="city">Winnipeg</settlement><region type="state">Manitoba</region></placeName></affiliation></author><author><name sortKey="Mukherjee, K" sort="Mukherjee, K" uniqKey="Mukherjee K" first="K" last="Mukherjee">K. Mukherjee</name></author><author><name sortKey="Geiger, J D" sort="Geiger, J D" uniqKey="Geiger J" first="J D" last="Geiger">J D Geiger</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="1996">1996</date><idno type="RBID">pubmed:8836637</idno><idno type="pmid">8836637</idno><idno type="wicri:Area/PubMed/Corpus">001870</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">001870</idno><idno type="wicri:Area/PubMed/Curation">001870</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">001870</idno><idno type="wicri:Area/PubMed/Checkpoint">001870</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">001870</idno><idno type="wicri:Area/Ncbi/Merge">002548</idno><idno type="wicri:Area/Ncbi/Curation">002548</idno><idno type="wicri:Area/Ncbi/Checkpoint">002548</idno><idno type="wicri:doubleKey">0014-2999:1996:Parkinson F:h:adenosine:transport</idno><idno type="wicri:Area/Main/Merge">004342</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">[3H]adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline.</title><author><name sortKey="Parkinson, F E" sort="Parkinson, F E" uniqKey="Parkinson F" first="F E" last="Parkinson">F E Parkinson</name><affiliation wicri:level="4"><nlm:affiliation>Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg, Canada.</nlm:affiliation><country xml:lang="fr">Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg</wicri:regionArea><orgName type="university">Université du Manitoba</orgName><placeName><settlement type="city">Winnipeg</settlement><region type="state">Manitoba</region></placeName></affiliation></author><author><name sortKey="Mukherjee, K" sort="Mukherjee, K" uniqKey="Mukherjee K" first="K" last="Mukherjee">K. Mukherjee</name></author><author><name sortKey="Geiger, J D" sort="Geiger, J D" uniqKey="Geiger J" first="J D" last="Geiger">J D Geiger</name></author></analytic><series><title level="j">European journal of pharmacology</title><idno type="ISSN">0014-2999</idno><imprint><date when="1996" type="published">1996</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Adenosine (metabolism)</term><term>Animals</term><term>Binding Sites</term><term>Biological Transport (drug effects)</term><term>Cricetinae</term><term>Dilazep (pharmacology)</term><term>Dipyridamole (pharmacology)</term><term>Genital Neoplasms, Male (metabolism)</term><term>Kinetics</term><term>Leiomyosarcoma (metabolism)</term><term>Leukemia L1210 (metabolism)</term><term>Male</term><term>Mesocricetus</term><term>Muscle, Smooth (drug effects)</term><term>Muscle, Smooth (metabolism)</term><term>Rats</term><term>Thioinosine (analogs & derivatives)</term><term>Thioinosine (metabolism)</term><term>Thioinosine (pharmacology)</term><term>Tumor Cells, Cultured</term><term>Vas Deferens (drug effects)</term><term>Vas Deferens (metabolism)</term><term>Xanthines (metabolism)</term><term>Xanthines (pharmacology)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Thioinosine</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Adenosine</term><term>Thioinosine</term><term>Xanthines</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Biological Transport</term><term>Muscle, Smooth</term><term>Vas Deferens</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Genital Neoplasms, Male</term><term>Leiomyosarcoma</term><term>Leukemia L1210</term><term>Muscle, Smooth</term><term>Vas Deferens</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Dilazep</term><term>Dipyridamole</term><term>Thioinosine</term><term>Xanthines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Binding Sites</term><term>Cricetinae</term><term>Kinetics</term><term>Male</term><term>Mesocricetus</term><term>Rats</term><term>Tumor Cells, Cultured</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">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.</div></front></TEI></record>Pour manipuler ce document sous Unix (Dilib)
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