Siguazodan 是选择性的，口服有效的磷酸二酯酶 III 抑制剂，IC50为 117 nM。它可增加完整血小板中 cAMP 的积累，EC50为 18.88 μM。它也抑制苯肾上腺素诱导的 5-HT 释放，IC50为 4.2 μM。

Siguazodan is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM。 Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM。

the major cyclic AMP-hydrolysing PDE in human platelet supernatantsselectively inhibited by Siguazodan . 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. 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[2].

Siguazodan is a selective phosphodiesterase III inhibitor that has positive inotropic and vasodilating actions in various laboratory animals and is orally active with a long duration of action in conscious dogs[2].

115344-47-3

C14H16N6O

284.32

SKF 94836

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years