4-[((1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル)メチル]-2-[4-[[(1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル]メチル]フェノキシ]フェノール

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P330：口をすすぐこと。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

  P362：汚染された衣類を脱ぎ、再使用す場合には洗濯をすること。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

4-[((1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル)メチル]-2-[4-[[(1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル]メチル]フェノキシ]フェノール 価格

4-[((1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル)メチル]-2-[4-[[(1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル]メチル]フェノキシ]フェノール 化学特性,用途語,生産方法

• 説明

  Dauricine is a kind of phenolic aromatic compound which is isolated from Menispermaceae plants such as Asian Menispermum dauricum or Canadian Menispermum dauricum and can be classified as isoquinoline alkaloids.
  Rhizoma Menispermi is the dry rhizome of Menispermaceae plant Menispermum dauricum. Menispermum dauricum mainly distributes in the northern part of East Asia and is mainly distributed in the north, east and northeast regions of China. The usage of Rhizoma Menispermi as a kind of traditional Chinese medicine was firstly recorded in Kaibao Herbs with its function of detoxifying many drugs, relieving pains, reducing swelling and sore, curing fever and cough, and killing parasites. According to the Chinese Pharmacopoeia, Rhizoma Menispermi in the north of China is different from the herbs used in the south of China known as the same name. Based on the traditional Chinese Medicine theory, Rhizoma Menispermi has the feature of bitterness and coldness, with the meridian tropism in the lung, stomach, and intestine. The main effects of Rhizoma Menispermi are heat-clearing, detoxicating, wind-dispelling and pain-relieving according to its vital function lies in the therapy of swollen sore throat, enteritis diarrhea and rheumatic arthralgia. Alkaloid is the main chemical component of Rhizoma Menispermi, and besides dauricine, there are also other kinds of alkaloids such as dauriciline, O-methyldauricine, and daurisoline in it.

• 物理的性質

  Appearance: yellowish-white powder or crystal. Solubility: soluble in ethanol, methanol, chloroform, acetone, benzene and slightly soluble in ether. Density: 1.185 g/cm3. Melting point: 115 °C. Boiling point: 712.3 °C at 760 mmHg atmospheric pressure. Specific optical rotation: MeOH-139.

• 来歴

  Menispermum dauricum has been long used as a traditional Chinese medicine, but the research of its effective components has been slow. Dauricine was firstly separated and structure-confirmed by Fukuda Mayo using alumina column chromatography separation assay in 1964. At the same year, dauricine was first synthesized by two Japanese scientists, Tetsuji Tamayama and Rtani Rikazu, by means of Arndt-Eistert reaction and Bischler-Napieralski reaction. Thereafter, lots of scientists from various countries successively separated daurinoline, Menispermum Xinlin alkali, Menispermum succinylcholine alkali, chelilanthifoline, stepholidine, and many other monomeric components of Menispermum dauricum.
  The study of dauricine in China started from the Cultural Revolution Period. Under the guidance of integrated traditional Chinese and Western medicine, a large number of effective components in traditional Chinese herbs were extracted, separated and applied to clinic. Dauricine was firstly reported on the mainland as an active ingredient in herbs which can clear away heat and toxic materials. Moreover, dauricine was also used as an antineoplastic and muscle relaxant. There were many medicines whose principal component was dauricine had been under clinical research for its role of cardiovascular protection since the 1980s, most of these medicines were stagnating in phase II clinical trials.

• 使用

  Dauricine is a bisbenzylisoquinoline allkaloid derivative that displays a noted number of pharmaceutical properties. It is known to induces severe lung toxicity in animals.

• 適応症

  Drugs whose main component is dauricine are still in clinical trials. Several formulations of dauricine have currently been developed, including tablets, capsules, injections, and so on. The main indications of dauricine in clinical trials are antiplatelet,antihypertensive and anti-arrhythmic.

• 定義

  ChEBI: A bisbenzylisoquinoline alkaloid resulting from the formal oxidative dimerisation of 4-{[(1R)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl]methyl}phenol by attachment of the phenolic oxygen of one molecule to the benzene ring f the second (ortho to the phenolic hydroxy group of the latter).

• 薬理学

  The main pharmacological actions of dauricine are as follows; Anti-arrhythmia: Dauricine can slow the heart rate and prolong conduction time in sinus rhythm, therefore reducing the incidence of arrhythmia.
  Anti-myocardial ischemia: Dauricine has protective effect on myocardial ischemia and can improve hemodynamic disturbances during ischemia which is supposed to produce effect via mechanism of improving myocardial metabolism and anti-oxidation.
  Anti-cerebral ischemia: Dauricine has an effective regulation on gene expression of Bcl-2 and Bax in cortical neurons after the ischemic brain injury, protecting against cerebral ischemia.
  Anti-cerebral ischemia/reperfusion injury: Dauricine can inhibit apoptosis induced by cerebral ischemia/reperfusion injury by upregulating Bcl-2 expression and downregulating Bax expression. Also dauricine has the effect of anti-oxidation.
  Antitumor activity: Dauricine can affect TGF-beta signaling pathway via upregulating gene expression of DPC4, and then the gene expression of P53 and P16 in tumor tissue, and finally reduce the gene expression of hFGF in tumor tissue. Thereby, the growth of various tumor cells could be inhibited.
  The investigations of metabolism in vivo of dauricine indicate that it is rapidly and widely distributed in body and the drug concentration in organs is significantly higher than that in plasma, and this is possibly related to its strong lipid solubility and easy access to cells.

• 臨床応用

  No medicine in the market takes dauricine as the main component up till now. Many animal experiments and clinical studies suggest that dauricine can reverse the effect of MDR as verapamil. Since the clinical application of the classical drug verapamil is limited for the serious toxic side effects, the moderate pharmacological effect of dauricine has a vital clinical significance. The main side effect of dauricine by oral absorption is gastrointestinal reaction, such as diarrhea, nausea, abdominal distension, and so on. In addition, dauricine can accumulate in the body, leading to hepatorenal toxicity and central nervous system toxicity.

4-[((1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル)メチル]-2-[4-[[(1R)-1,2,3,4-テトラヒドロ-6,7-ジメトキシ-2-メチルイソキノリン-1-イル]メチル]フェノキシ]フェノール 生産企業

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