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Siguazodan

CAS No. : 115344-47-3

MCE 站：Siguazodan

产品活性：Siguazodan (SKF 94836) 是一种有效的，选择性的，口服活性的磷酸二酯酶 III (PDE-III) 抑制剂，IC₅₀ 为 117 nM。Siguazodan 可增加完整血小板中 cAMP 的积累，EC₅₀ 为 18.88 μM。Siguazodan 还抑制苯肾上腺素诱导的 5-HT 释放，IC₅₀ 值为 4.2 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphodiesterase (PDE)

In Vitro: Siguazodan selectively inhibits the major cyclic AMP-hydrolysing PDE in human platelet supernatants. The inhibited enzyme has been variously termed cyclic GMP-inhibited PDE or PDE-III. In platelet-rich plasma (PRP), Siguazodan inhibits U46619-induced aggregation more potently than that induced by adenosine 5'-diphosphate (ADP), and collagen. Treatment of the PRP with Aspirin has no effect on the potency of Siguazodan. In washed platelets, Siguazodan increases cyclic AMP levels and reduces cytoplasmic free calcium. ADP decreases the ability of Siguazodan to raise cyclic AMP and this may explain its lower potency in inhibiting responses to ADP. Siguazodan has anti-platelet actions over the same concentration range that it is an inotrope and vasodilator.

In Vivo: Siguazodan is a potent, selective inhibitor of phosphodiesterase III that has positive inotropic and vasodilating actions in various laboratory animals and is orally active with a long duration of action in conscious dogs.

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