[3H]Adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline
Identifieur interne : 003D22 ( Main/Exploration ); précédent : 003D21; suivant : 003D23[3H]Adenosine transport in DDT1 MF-2 smooth muscle cells: inhibition by metabolites of propentofylline
Auteurs : Fiona E. Parkinson [Canada] ; Kallol Mukherjee [Canada] ; Jonathan D. Geiger [Canada]Source :
- 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 (±)-A72 0287. Based on recent findings that some transport inhibitors exhibit marked stereoselectivity, we tested the degree to which individual stereoisomers of (±)-A72 0287 affect adenosine transport. Propentofylline inhibited [3H]adenosine transport in DDT1 MF-2 cells with an IC50 value of 24 μM. (±)-A72 0287 and the individual stereoisomeers (+)-83 3791 and (−)-84 4261 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.
Url:
DOI: 10.1016/0014-2999(96)00259-2
Affiliations:
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Le document en format XML
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Parkinson</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, University of Manitoba, 770 Bannatyne Avenue, 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, Kallol" sort="Mukherjee, Kallol" uniqKey="Mukherjee K" first="Kallol" last="Mukherjee">Kallol Mukherjee</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, University of Manitoba, 770 Bannatyne Avenue, 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="Geiger, Jonathan D" sort="Geiger, Jonathan D" uniqKey="Geiger J" first="Jonathan D." last="Geiger">Jonathan D. Geiger</name><affiliation wicri:level="4"><country>Canada</country><wicri:regionArea>Department of Pharmacology and Therapeutics, University of Manitoba, 770 Bannatyne Avenue, Winnipeg</wicri:regionArea><orgName type="university">Université du Manitoba</orgName><placeName><settlement type="city">Winnipeg</settlement><region type="state">Manitoba</region></placeName></affiliation></author></analytic><monogr></monogr><series><title level="j">European Journal of Pharmacology</title><title level="j" type="abbrev">EJP</title><idno type="ISSN">0014-2999</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1996">1996</date><biblScope unit="volume">308</biblScope><biblScope unit="issue">1</biblScope><biblScope unit="page" from="97">97</biblScope><biblScope unit="page" to="102">102</biblScope></imprint><idno type="ISSN">0014-2999</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0014-2999</idno></seriesStmt></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><langUsage><language ident="en">en</language></langUsage></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 (±)-A72 0287. Based on recent findings that some transport inhibitors exhibit marked stereoselectivity, we tested the degree to which individual stereoisomers of (±)-A72 0287 affect adenosine transport. Propentofylline inhibited [3H]adenosine transport in DDT1 MF-2 cells with an IC50 value of 24 μM. (±)-A72 0287 and the individual stereoisomeers (+)-83 3791 and (−)-84 4261 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><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><country name="Canada"><region name="Manitoba"><name sortKey="Parkinson, Fiona E" sort="Parkinson, Fiona E" uniqKey="Parkinson F" first="Fiona E." last="Parkinson">Fiona E. Parkinson</name></region><name sortKey="Geiger, Jonathan D" sort="Geiger, Jonathan D" uniqKey="Geiger J" first="Jonathan D." last="Geiger">Jonathan D. Geiger</name><name sortKey="Mukherjee, Kallol" sort="Mukherjee, Kallol" uniqKey="Mukherjee K" first="Kallol" last="Mukherjee">Kallol Mukherjee</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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