ジヒドロエルゴトキシンメシル酸塩 化学特性,用途語,生産方法
外観
白色～うすい黄色、結晶性粉末～粉末
用途
麦角アルカロイドのエルゴト
キシン（エルゴコルニン、エルゴクリスチン、
エルゴクリプチンの混合物）をジヒドロ化し
た化合物です。エルゴトキシンに比べて強い
α 遮断作用を示します。
効能
向知性薬, 血管拡張薬, αアドレナリン受容体拮抗薬
説明
Ergoloid, also known as dihydroergotoxine mesylate, is a mixture of the ergot alkaloids dihydroergocornine, dihydroergocrystine, and dihydroergocryptine. It blocks reflex vasodilation and vasoconstriction induced by norepinephrine in dogs when injected into the kidney at a dose of 0.15 mg. Ergoloid blocks norepinephrine-induced cAMP production in rat brain cortical homogenates
ex vivo in a dose-dependent manner. It also acts as an erectogenic agent in rats. Formulations containing ergoloid have been used in the treatment of migraine headaches and vascular dementias.
使用
Cognition adjuvant. Dihydroergotoxine mesylate binds with high affinity to GABAA receptor Cl- channel. Interacts with central dopaminergic, serotonergic and adrenergic (a1) receptors. Exhibits antirproliferative activity in vitro. Displays cognition-enhancing, anticonvulsant and sedative activity in vivo. Dihydroergotoxine mesylate is a substrate of GABA Receptor.
定義
ChEBI: Dihydroergotoxine mesylate is a mixture of hydrogenated ergot alkaloids consisting of the methanesulfonic acid salts of dihydroergocornine (R = CHMe2), dihydroergocristine (R = CH2Ph), and alpha- and beta-dihydroer ocryptine (R = CH2CHMe2 and CH(Me)Et, respectively). It is used for the symptomatic treatment of mild to moderate dementia in the elderly, although its value is not established.
生物活性
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts. Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site. Also interacts with central dopaminergic, serotonergic and adrenergic (α1) receptors. Displays antiproliferative activity in vitro (IC50 = 18 - 38 μM in prostate cancer cells) and exhibits cognition-enhancing, anticonvulsant and sedative activity in vivo.
ジヒドロエルゴトキシンメシル酸塩 上流と下流の製品情報
原材料
準備製品