Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.
Identifieur interne : 003860 ( Main/Exploration ); précédent : 003859; suivant : 003861Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.
Auteurs : S L Borgland [Canada] ; M. Casta N ; W. Spevak ; F E ParkinsonSource :
- Canadian journal of physiology and pharmacology [ 0008-4212 ] ; 1998.
English descriptors
- KwdEn :
- Adenosine (pharmacology), Animals, CHO Cells, Colforsin (pharmacology), Cricetinae, Genes, Reporter (drug effects), Humans, Luciferases (biosynthesis), Luciferases (drug effects), Luciferases (genetics), Neuroprotective Agents (pharmacology), Purinergic P1 Receptor Antagonists, Receptor, Adenosine A2A, Receptor, Adenosine A2B, Receptors, Purinergic P1 (drug effects), Receptors, Purinergic P1 (genetics), Transfection, Xanthines (pharmacology).
- MESH :
- chemical , biosynthesis : Luciferases.
- chemical , drug effects : Luciferases, Receptors, Purinergic P1.
- chemical , genetics : Luciferases, Receptors, Purinergic P1.
- chemical , pharmacology : Adenosine, Colforsin, Neuroprotective Agents, Xanthines.
- drug effects : Genes, Reporter.
- Animals, CHO Cells, Cricetinae, Humans, Purinergic P1 Receptor Antagonists, Receptor, Adenosine A2A, Receptor, Adenosine A2B, Transfection.
Abstract
Propentofylline is neuroprotective in vivo, but its mechanism of action is not completely understood. Previously, propentofylline was shown to block adenosine transport processes, to inhibit three adenosine receptor subtypes, and to inhibit cAMP phosphodiesterase. We tested the effect of propentofylline on adenosine receptor function in Chinese hamster ovary (CHO) cells transfected with human adenosine A1, A2A, or A2B receptors and a luciferase reporter gene under control of a promoter sequence containing several copies of the cAMP response element. We investigated the concentration-dependent inhibitory effects of propentofylline on cAMP phosphodiesterase, adenosine transport processes, and adenosine A1, A2A, and A2B receptors. At concentrations > or = 1 mM, propentofylline increased luciferase activity probably as a result of inhibition of cAMP phosphodiesterase. Inhibition of [3H]adenosine uptake by propentofylline was concentration dependent, with IC50 values of 37-39 microM for the three cell types. Agonist-activated adenosine A1 receptors were antagonized by 100 microM propentofylline, but inhibition of agonist-stimulated A2A or A2B receptors was not observed. In contrast, A1 and A2A receptor mediated effects of adenosine were enhanced by propentofylline at concentrations of 1 and 100 microM, respectively. These data indicate that the net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present.
PubMed: 10326835
Affiliations:
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Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.</title><author><name sortKey="Borgland, S L" sort="Borgland, S L" uniqKey="Borgland S" first="S L" last="Borgland">S L Borgland</name><affiliation wicri:level="4"><nlm:affiliation>Department of Pharmacology and Therapeutics, The University of Manitoba, Winnipeg, Canada.</nlm:affiliation><country xml:lang="fr">Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, The 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="Casta N, M" sort="Casta N, M" uniqKey="Casta N M" first="M" last="Casta N">M. Casta N</name></author><author><name sortKey="Spevak, W" sort="Spevak, W" uniqKey="Spevak W" first="W" last="Spevak">W. Spevak</name></author><author><name sortKey="Parkinson, F E" sort="Parkinson, F E" uniqKey="Parkinson F" first="F E" last="Parkinson">F E Parkinson</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="1998">1998</date><idno type="RBID">pubmed:10326835</idno><idno type="pmid">10326835</idno><idno type="wicri:Area/PubMed/Corpus">001740</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">001740</idno><idno type="wicri:Area/PubMed/Curation">001740</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">001740</idno><idno type="wicri:Area/PubMed/Checkpoint">001740</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">001740</idno><idno type="wicri:Area/Ncbi/Merge">000019</idno><idno type="wicri:Area/Ncbi/Curation">000019</idno><idno type="wicri:Area/Ncbi/Checkpoint">000019</idno><idno type="wicri:doubleKey">0008-4212:1998:Borgland S:effects:of:propentofylline</idno><idno type="wicri:Area/Main/Merge">003E69</idno><idno type="wicri:Area/Main/Curation">003860</idno><idno type="wicri:Area/Main/Exploration">003860</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene.</title><author><name sortKey="Borgland, S L" sort="Borgland, S L" uniqKey="Borgland S" first="S L" last="Borgland">S L Borgland</name><affiliation wicri:level="4"><nlm:affiliation>Department of Pharmacology and Therapeutics, The University of Manitoba, Winnipeg, Canada.</nlm:affiliation><country xml:lang="fr">Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, The 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="Casta N, M" sort="Casta N, M" uniqKey="Casta N M" first="M" last="Casta N">M. Casta N</name></author><author><name sortKey="Spevak, W" sort="Spevak, W" uniqKey="Spevak W" first="W" last="Spevak">W. Spevak</name></author><author><name sortKey="Parkinson, F E" sort="Parkinson, F E" uniqKey="Parkinson F" first="F E" last="Parkinson">F E Parkinson</name></author></analytic><series><title level="j">Canadian journal of physiology and pharmacology</title><idno type="ISSN">0008-4212</idno><imprint><date when="1998" type="published">1998</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Adenosine (pharmacology)</term><term>Animals</term><term>CHO Cells</term><term>Colforsin (pharmacology)</term><term>Cricetinae</term><term>Genes, Reporter (drug effects)</term><term>Humans</term><term>Luciferases (biosynthesis)</term><term>Luciferases (drug effects)</term><term>Luciferases (genetics)</term><term>Neuroprotective Agents (pharmacology)</term><term>Purinergic P1 Receptor Antagonists</term><term>Receptor, Adenosine A2A</term><term>Receptor, Adenosine A2B</term><term>Receptors, Purinergic P1 (drug effects)</term><term>Receptors, Purinergic P1 (genetics)</term><term>Transfection</term><term>Xanthines (pharmacology)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="biosynthesis" xml:lang="en"><term>Luciferases</term></keywords><keywords scheme="MESH" type="chemical" qualifier="drug effects" xml:lang="en"><term>Luciferases</term><term>Receptors, Purinergic P1</term></keywords><keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>Luciferases</term><term>Receptors, Purinergic P1</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Adenosine</term><term>Colforsin</term><term>Neuroprotective Agents</term><term>Xanthines</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Genes, Reporter</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>CHO Cells</term><term>Cricetinae</term><term>Humans</term><term>Purinergic P1 Receptor Antagonists</term><term>Receptor, Adenosine A2A</term><term>Receptor, Adenosine A2B</term><term>Transfection</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Propentofylline is neuroprotective in vivo, but its mechanism of action is not completely understood. Previously, propentofylline was shown to block adenosine transport processes, to inhibit three adenosine receptor subtypes, and to inhibit cAMP phosphodiesterase. We tested the effect of propentofylline on adenosine receptor function in Chinese hamster ovary (CHO) cells transfected with human adenosine A1, A2A, or A2B receptors and a luciferase reporter gene under control of a promoter sequence containing several copies of the cAMP response element. We investigated the concentration-dependent inhibitory effects of propentofylline on cAMP phosphodiesterase, adenosine transport processes, and adenosine A1, A2A, and A2B receptors. At concentrations > or = 1 mM, propentofylline increased luciferase activity probably as a result of inhibition of cAMP phosphodiesterase. Inhibition of [3H]adenosine uptake by propentofylline was concentration dependent, with IC50 values of 37-39 microM for the three cell types. Agonist-activated adenosine A1 receptors were antagonized by 100 microM propentofylline, but inhibition of agonist-stimulated A2A or A2B receptors was not observed. In contrast, A1 and A2A receptor mediated effects of adenosine were enhanced by propentofylline at concentrations of 1 and 100 microM, respectively. These data indicate that the net effects of propentofylline in vivo will be dependent on the concentrations of propentofylline and adenosine available and on the subtypes of adenosine receptors, phosphodiesterases, and nucleoside transporters present.</div></front></TEI><affiliations><list><country><li>Canada</li></country><region><li>Manitoba</li></region><settlement><li>Winnipeg</li></settlement><orgName><li>Université du Manitoba</li></orgName></list><tree><noCountry><name sortKey="Casta N, M" sort="Casta N, M" uniqKey="Casta N M" first="M" last="Casta N">M. Casta N</name><name sortKey="Parkinson, F E" sort="Parkinson, F E" uniqKey="Parkinson F" first="F E" last="Parkinson">F E Parkinson</name><name sortKey="Spevak, W" sort="Spevak, W" uniqKey="Spevak W" first="W" last="Spevak">W. Spevak</name></noCountry><country name="Canada"><region name="Manitoba"><name sortKey="Borgland, S L" sort="Borgland, S L" uniqKey="Borgland S" first="S L" last="Borgland">S L Borgland</name></region></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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