Cardiovascular effects of BRX-005: Comparison to bimoclomol

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• 作者：Kö ; rtvé ; ly ; Á ; gnes ; Szigeti ; Gyula ; Gesztelyi ; Rudolf ; Zsuga ; Judit ; Bá ; nyá ; sz ; Tamá ; s ; et. al.
• 关键词：Heat shock protein ; Heart ; Positive inotropic drugs ; Intracellular calcium transients ; Calcium sensitizers ; Bimoclomol
• 刊名：Life Sciences
• 出版年：2000
• 出版时间：August 25, 2000
• 年：2000
• 卷：67
• 期：14
• 页码：1783-1789
• 全文大小：187 K

文摘

Concentration-dependent effects of BRX-005, the novel heat shock protein coinducer, cardioprotective and vasoprotective agent, on intracellular calcium transients and contractility were studied in Langendorff-perfused guinea pig hearts loaded with the fluorescent calcium indicator dye Fura-2. BRX-005 increased peak left ventricular pressure, the rate of force development and relaxation significantly in a concentration-dependent manner. The amplitude of [Ca²+]_i transients was left unaltered by the drug. In contrast to BRX-005, bimoclomol increased both contractility and the amplitude of [Ca²+]_i transients. In canine ventricular cardiomyocytes high concentrations of BRX-005 had no effect on depolarization, whereas bimoclomol suppressed action potential upstroke markedly. In guinea pig pulmonary artery preparations precontracted with phenylephrine, BRX-005 induced concentration-dependent relaxation. This effect of BRX-005 was independent of the integrity of endothelium indicating that vasorelaxant effect of the drug develops directly on vascular smooth muscle.