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新型正性肌力磷酸二酯酶抑制剂

The new inotropic phosphodiesterase inhibitors.

作者信息

el Allaf D, D'Orio V, Carlier J

出版信息

Arch Int Physiol Biochim. 1984 Nov;92(4):S69-79. doi: 10.3109/13813458409071165.

Abstract

Compounds with phosphodiesterase inhibitory activity stimulate myocardial contractility by increasing the intracellular cyclic AMP concentrations. They can also increase Ca2+ entry and inhibit Ca2+ sequestration by the sarcoplasmic reticulum. Xanthines produce bronchodilation with associated venous and arteriolar dilation. However, their use is limited by their positive chronotropic effect and other side effects at high plasma levels. New phosphodiesterase inhibitors have been perfected: they are more specific with little chronotropic effect. Increasing the sensitivity of the myofilaments to Ca2+, and other unclear mechanisms may be involved in the inotropic action of these drugs. These new promising active compounds are described and discussed. They augment cardiac performance and improve regional distribution of blood flow and symptoms. However, their influence on the long-term outcome of severe heart failure has yet to be determined.

摘要

具有磷酸二酯酶抑制活性的化合物通过增加细胞内环磷酸腺苷(cAMP)浓度来刺激心肌收缩力。它们还可增加钙离子(Ca2+)内流,并抑制肌浆网对Ca2+的摄取。黄嘌呤可引起支气管扩张,并伴有静脉和小动脉扩张。然而,其使用受到正性变时作用以及高血浆水平时其他副作用的限制。新型磷酸二酯酶抑制剂已得到完善:它们更具特异性,且变时作用较小。增加肌丝对Ca2+的敏感性以及其他尚不清楚的机制可能参与了这些药物的变力作用。本文对这些新的有前景的活性化合物进行了描述和讨论。它们可增强心脏功能,改善血流的区域分布和症状。然而,它们对严重心力衰竭长期预后的影响尚未确定。

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