Depressant effects of chloroquine on the isolated guinea-pig heart.
Depressant effects of chloroquine on the isolated guinea-pig heart.
复制标题
氯喹对离体豚鼠心脏的抑制作用。
DOI：
10.1016/0014-2999(90)90108-i
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发表时间：
1990
影响因子：
5
通讯作者：
Brody,TM
中科院分区：
文献类型：
--
作者：
Tona,L;Ng,YC;Akera,T;Brody,TM
一些抗疟疾药物对心脏有有害影响。我们比较了氯喹和奎尼克林对豚鼠心房和朗宁多夫制剂的作用，以评估它们对几个钙池的影响。两种化合物均以浓度(氯喹10-100μM；奎尼卡因3-100μM)和时间依赖的方式降低已发展的张力，且喹卡林的效力是氯喹的两倍。心室肌对氯喹的敏感性明显高于心房肌。氯喹的浓度与摄入中毒剂量的患者血清中的浓度相当，可显著抑制已形成的紧张。氯喹的洗脱作用几乎完全逆转；奎纳克林则不那么容易逆转。氯喹对部分去极化的心房标本也有直接的负性变时性作用，显著降低力频关系并产生张力；而哇巴因的静息后收缩和正性变力作用不受影响。细胞外钙的增加可拮抗负性变力作用。奎尼卡因对静息后收缩有明显作用，并可减弱哇巴因的正性变力作用。结果表明，氯喹的作用可能涉及一个表面的钙池，而喹卡林可能作用于多个钙池。
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.