ジピリダモール 化学特性,用途語,生産方法
外観
うすい黄色～黄色～黄赤色粉末～結晶
用途
冠血管拡張作用を示します。
効能
冠血管拡張薬, 血小板凝集抑制薬, ホスホジエステラーゼ阻害薬
商品名
ペルサンチン (日本ベーリンガーインゲルハイム); ペルサンチン (日本ベーリンガーインゲルハイム); ペルサンチン (日本ベーリンガーインゲルハイム); ペルサンチン (日本ベーリンガーインゲルハイム); ペルサンチン (日本ベーリンガーインゲルハイム)
化学的特性
Yellow Powder
使用
Dipyridamole prevents platelets sticking to the replacement heart valve and causing a blood clot on the valve. It is used to dilate blood vessels in people with peripheral arterial disease and coronary artery disease. This compound has been shown to suppress high glucose-induced osteopontin mRNA expression and protein secretion, as well as inhibit cAMP and cGMP hydrolysis. Research indicates that Dipyridamole is a non-specific nucleoside transport inhibitor with the ability to increase the effects of adenosine in sinoatrial and atrioventricular nodes. Dipyridamole is an inhibitor of ENT1 and ENT2.
定義
ChEBI: A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.
一般的な説明
Dipyridamole, 2,2',2',2'''-[(4,8-di-1piperidinylpyrimido[5,4-d]pyrimidine-2,6-diyl)dinitrilo]-tetrakisethanol (Persantine), may be used for coronary andmyocardial insufficiency. Its biggest use today, however, isas an antithrombotic in patients with prosthetic heart valves.It is a bitter, yellow, crystalline powder, soluble in diluteacids, methanol, or chloroform. A formulation containingdipyridamole and aspirin (Aggrenox) is currently beingmarketed as an antithromobotic.
Dipyridamole is a long-acting vasodilator. Its vasodilatingaction is selective for the coronary system; it is indicatedfor long-term therapy of chronic angina pectoris. Thedrug also inhibits adenosine deaminase in erythrocytesand interferes with the uptake of the vasodilator adenosineby erythrocytes. These actions potentiate the effect ofprostacyclin (PGI
2), which acts as an inhibitor to plateletaggregation.
生物活性
Coronary vasodilator; adenosine transport inhibitor. Phosphodiesterase inhibitor (IC 50 values are 0.37, 0.38, 0.45, 0.9 and 4.5 μ M? for PDE11, 6, 10, 5 and 8 respectively).
作用機序
Dipyridamole exerts its antiplatelet function by increasing cellular concentrations of cAMP
via its inhibition of the degradating enzyme, cyclic nucleotide PDE3. It also blocks adenosine
uptake, which acts at A2 adenosine receptors to stimulate platelet adenyl cyclase. Less common
uses for this drug include inhibition of embolization from prosthetic heart valves when used in
combination with warfarin (the only currently recommended use) and reduction of thrombosis in
patients with thrombotic disease when used in combination with aspirin. Alone, dipyridamole has
little, if any, benefit in the treatment of thrombotic conditions.
臨床応用
Dipyridamole is a pyrimidopyrimidine derivative with vasodilatory and antiplatelet properties.
安全性プロファイル
Poison by intraperitoneal and intravenous routes. Moderately toxic by ingestion and subcutaneous routes. Human systemic effects cardiomyopathy including infarction. Mutation data reported. Used as a coronary vasodilator. When heated to decomposition it e
ジピリダモール 上流と下流の製品情報
原材料
準備製品