Depressant effects of chloroquine on the isolated guinea-pig heart
Identifieur interne : 003080 ( Main/Exploration ); précédent : 003079; suivant : 003081Depressant effects of chloroquine on the isolated guinea-pig heart
Auteurs : Lutete Tona [États-Unis] ; Yuk-Chow Ng [États-Unis] ; Tai Akera [États-Unis] ; Theodore M. Brody [États-Unis]Source :
- European Journal of Pharmacology [ 0014-2999 ] ; 1990.
English descriptors
- KwdEn :
- Teeft :
- Atrial, Atrial muscle preparations, Atrium, Buffer solution, Calcium concentration, Calcium pools, Cardiac, Chloroquine, Contractile, Contractility, Different concentrations, Equilibration, Exchange system, Inotropic, Inotropic effect, Inotropic effects, Krebshenseleit buffer solution, Langendorff, Langendorff preparations, Myocardial contractility, Negative inotropic effect, Ouabain, Pharmacol, Physiol, Positive inotropic effect, Potentiated, Potentiated contraction, Present address, Present study, Quinacrine, Right atria, Sarcoplasmic reticulum, Ventricular, Ventricular muscle, Vertical lines.
Abstract
Some anti-malarials have deleterious effects upon the heart. The actions of two of these, chloroquine and quinacrine, were compared on isolated guinea-pig atria and Langendorff preparations to assess their effects on several calcium pools. Both compounds decreased developed tension in a concentration (chloroquine 10–100 μM; quinacrine 3–100 μM) and time-dependent manner, with quinacrine being twice as potent as chloroquine. Ventricular muscle was much more sensitive to chloroquine than was atrial muscle. Concentrations of chloroquine, comparable to that found in the serum of patients ingesting toxic doses, caused significant inhibition of developed tension. The effects of chloroquine were almost completely reversed on washout; quinacrine, however, was less readily reversible. Chloroquine also had a direct negative chronotropic effect, substantially reduced force-frequency relationships and developed tension in partially depolarized atrial preparations; while post-rest contraction and the positive inotropic effect of ouabain were unaffected. Increases in extracellular calcium antagonized the negative inotropic effect. Quinacrine had a marked effect on post-rest contraction and attenuated the positive inotropic action of ouabain. It is concluded that the action of chloroquine may involve a superficial calcium pool, while quinacrine may act upon several calcium pools.
Url:
DOI: 10.1016/0014-2999(90)90108-I
Affiliations:
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Brody</name><affiliation wicri:level="4"><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmacology and Toxicology, Michigan State University, East Lansing, MI 48824</wicri:regionArea><placeName><region type="state">Michigan</region><settlement type="city">East Lansing</settlement></placeName><orgName type="university">Université d'État du Michigan</orgName></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="1990">1990</date><biblScope unit="volume">178</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="293">293</biblScope><biblScope unit="page" to="301">301</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>(Guinea-pig)</term><term>Ca2+</term><term>Cardiac contraction</term><term>Chloroquine</term><term>Quinacrine</term></keywords><keywords scheme="Teeft" xml:lang="en"><term>Atrial</term><term>Atrial muscle preparations</term><term>Atrium</term><term>Buffer solution</term><term>Calcium concentration</term><term>Calcium pools</term><term>Cardiac</term><term>Chloroquine</term><term>Contractile</term><term>Contractility</term><term>Different concentrations</term><term>Equilibration</term><term>Exchange system</term><term>Inotropic</term><term>Inotropic effect</term><term>Inotropic effects</term><term>Krebshenseleit buffer solution</term><term>Langendorff</term><term>Langendorff preparations</term><term>Myocardial contractility</term><term>Negative inotropic effect</term><term>Ouabain</term><term>Pharmacol</term><term>Physiol</term><term>Positive inotropic effect</term><term>Potentiated</term><term>Potentiated contraction</term><term>Present address</term><term>Present study</term><term>Quinacrine</term><term>Right atria</term><term>Sarcoplasmic reticulum</term><term>Ventricular</term><term>Ventricular muscle</term><term>Vertical lines</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Some anti-malarials have deleterious effects upon the heart. The actions of two of these, chloroquine and quinacrine, were compared on isolated guinea-pig atria and Langendorff preparations to assess their effects on several calcium pools. Both compounds decreased developed tension in a concentration (chloroquine 10–100 μM; quinacrine 3–100 μM) and time-dependent manner, with quinacrine being twice as potent as chloroquine. Ventricular muscle was much more sensitive to chloroquine than was atrial muscle. Concentrations of chloroquine, comparable to that found in the serum of patients ingesting toxic doses, caused significant inhibition of developed tension. The effects of chloroquine were almost completely reversed on washout; quinacrine, however, was less readily reversible. Chloroquine also had a direct negative chronotropic effect, substantially reduced force-frequency relationships and developed tension in partially depolarized atrial preparations; while post-rest contraction and the positive inotropic effect of ouabain were unaffected. Increases in extracellular calcium antagonized the negative inotropic effect. Quinacrine had a marked effect on post-rest contraction and attenuated the positive inotropic action of ouabain. It is concluded that the action of chloroquine may involve a superficial calcium pool, while quinacrine may act upon several calcium pools.</div></front></TEI><affiliations><list><country><li>États-Unis</li></country><region><li>Michigan</li></region><settlement><li>East Lansing</li></settlement><orgName><li>Université d'État du Michigan</li></orgName></list><tree><country name="États-Unis"><region name="Michigan"><name sortKey="Tona, Lutete" sort="Tona, Lutete" uniqKey="Tona L" first="Lutete" last="Tona">Lutete Tona</name></region><name sortKey="Akera, Tai" sort="Akera, Tai" uniqKey="Akera T" first="Tai" last="Akera">Tai Akera</name><name sortKey="Brody, Theodore M" sort="Brody, Theodore M" uniqKey="Brody T" first="Theodore M." last="Brody">Theodore M. Brody</name><name sortKey="Ng, Yuk Chow" sort="Ng, Yuk Chow" uniqKey="Ng Y" first="Yuk-Chow" last="Ng">Yuk-Chow Ng</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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