AP-155(AP-155) - 药物靶点：PDE1C_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

PDE1C

作用机制

PDE1C抑制剂(phosphodiesterase 1C inhibitors)、血小板聚集抑制剂

治疗领域

心血管疾病

在研适应症-

非在研适应症

心肌缺血血栓形成

原研机构

University of Genova

在研机构-

非在研机构

University of Genova

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 AP-155 相关的临床结果

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100 项与 AP-155 相关的转化医学

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100 项与 AP-155 相关的专利（医药）

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1

项与 AP-155 相关的文献（医药）

1997-06-01·Biochemical Pharmacology2区 · 医学

Effect of 2(1-piperazinyl)-4H-pyrido[1,2-a]pyrimidin-4-one (AP155) on human platelets in vitro

2区 · 医学

Article

作者: Giuliana Leoncini ; Giorgio Roma ; Mario Di Braccio ; Maria Gracia Signorello

The effect on human platelets of 2-(1-piperazinyl)-4H-pyrido[1,2-a]pyrimi din-4-one (AP155) was tested in vitro by measuring cyclic adenosine monophosphate (cAMP) level, cytosolic Ca++, [(125I)]fibrinogen binding as well as aggregation induced by several agonists. AP155 dose-dependently inhibited aggregation both in platelet rich plasma (PRP) and in washed platelets (WP), exerting its maximal power in the presence of collagen, ADP and platelet activating factor (PAF). It specifically inhibited the activity of cAMP high affinity phosphodiesterase (PDE), resulting in a sufficient increase in cAMP levels to activate cAMP-dependent protein kinase. AP155 was able to inhibit aggregation, the increase in cytosolic Ca++ induced by thrombin, and fibrinogen binding to ADP or thrombin-stimulated platelets. Thus, this new pyridopyrimidine derivative exerts its antiplatelet activity by increasing cAMP intracellular concentration.

100 项与 AP-155 相关的药物交易

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