ナルフラフィン塩酸塩

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

  H336：眠気やめまいのおそれ

• 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。

  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。

  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。

  P312：気分が悪い時は医師に連絡すること。

  P330：口をすすぐこと。

  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。

ナルフラフィン塩酸塩 化学特性,用途語,生産方法

• 効能

  鎮痒薬, κ-オピオイド受容体作動薬

• 商品名

  レミッチ (東レ); レミッチ (東レ)

• 説明

  Pruritus (chronic itching) is a common symptom seen in 25-90% of uremic patients, especially those with chronic renal failure requiring hemodialysis. Nalfurafine hydrochloride is a new member of this class that exhibits an improved safety profile as compared with its predecessors in preclinical studies. It is a potent agonist for the κ-opioid receptor (K_i = 0.24 nM, EC₅₀ = 0.008 nM, I_max = 91%), with substantially lower binding and agonism of the - or d-opioid receptors (K_i = 2.24 and 484 nM, EC₅₀ = 1.66 and 21.3 nM, I_max = 53 and 78%, respectively). In vivo, nalfurafine hydrochloride demonstrates potent antipruritic activity against histamine-sensitive as well as histamine-resistant itch in mouse pruritogen-induced scratching models.
  The most common adverse event associated with nalfurafine hydrochloride was insomnia or sleep disturbance, seen in 10% of the treated patients. Nalfurafine is structurally related to naltrexone (Revia ), an opioid receptor antagonist marketed for treating alcohol dependence. Nalfurafine is synthesized in two steps starting from naltrexone, via reductive amination with methylamine under catalytic hydrogenation conditions, and subsequent acylation with 3(E)-(3-furyl) acryloyl chloride.

• 使用

  Nalfurafine hydrochloride was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by hemodialysis. It showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. A new therapeutic agent for the treatment of uremic pruritus in hemodialysis patients.

ナルフラフィン塩酸塩 生産企業

Global(67)Suppliers

152658-17-8, ナルフラフィン塩酸塩 キーワード