1-ヒドラジノフタラジン塩酸塩

解説1-hydrazinophthalazine monohydrochloride．C8H8N4HCl(196.64)．ヒドララジン塩酸塩, 1-クロロフタラジンにヒドラジンヒドラートを反応させると得られる．塩酸塩は分解点273 ℃．λmax 211，240，260，304，315 nm(水)．水に可溶，エタノールに難溶．血管の拡張による血圧低下作用を有し，抗高血圧症薬として使用される．種々の副作用を伴うので，長期投与には注意を要する．LD50 34 mg/kg(ラット，静注)．森北出版「化学辞典（第2版）

用途降圧剤?血管拡張剤

用途有機合成原料。

説明Hydralazine is an orally bioavailable vasodilator and antihypertensive agent. It decreases DNA methylation in Jurkat cells at a concentration of 10 μM and inhibits extracellular and intracellular production of reactive oxygen species (ROS) in rat macrophages activated by phorbol 12-myristate 13-acetate (PMA; ) at a concentration of 100 μM. Hydralazine (100 μM) also decreases nitric oxide production and mRNA expression of inducible nitric oxide synthase (iNOS) in rat macrophages activated by LPS (Item Nos. 19660| 19661| 19662) and interferon-γ (IFN-γ). It reduces contraction of rat aortic arterial strips induced by potassium and norepinephrine (; IC50s = 2.2 and 3.06 mM, respectively). Hydralazine (2.6 mg/kg) lowers mean arterial blood pressure (MAP) by 41.76% in conscious rats. Formulations containing hydralazine have been used in the treatment of high blood pressure and heart failure.

使用Hydralazine hydrochloride has been used:as a vasodilator to study its effects on hypertension in T-cell frequencies in juvenile ratsas a semicarbazide-sensitive amine oxidase (SSAO) inhibitor to study its effects on myocardial ischemia-reperfusion (I/R) injuryas a vasodilator to study its effects on insulin secretion and glucose tolerance

一般的な説明Hydralazine hydrochloride,1-hydrazinophthalazine monohydrochloride(Apresoline hydrochloride), originated from the work of achemist attempting to produce some unusual chemicalcompounds and from the observation that this compoundhad antihypertensive properties. It occurs as yellow crystalsand is soluble in water to the extent of about 3%. A 2%aqueous solution has a pH of 3.5 to 4.5.