4-アミノサリチル酸

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

  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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ 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。

  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。

  P405：施錠して保管すること。

4-アミノサリチル酸 価格

MSDS Information

• PAS

4-アミノサリチル酸 化学特性,用途語,生産方法

• 外観

  白色～わずかにうすい褐色, 結晶性粉末～粉末

• 溶解性

  エタノールに溶け、水にほとんど溶けない。

• 解説

  フクシンアルデヒド試薬(fuchsin-aldehyde reagent)ともいう．ドイツの有機化学者H. Schiffによって創案された．アルデヒドの検出試薬として有名であり，アルデヒドとケトンを判別する目的で用いられることが多い．フクシン0.2 g を水200 mL に溶解，これに亜硫酸15 mL を加えて一夜放置すると，脱色されて無色になる．この試薬1滴をアルデヒドの検液に加えて振ると，室温で反応して赤紫色を呈する．しかし，ケトンはこの反応がみられない．この反応はアルデヒドに対しては鋭敏な呈色反応である．
  森北出版「化学辞典（第2版）

• 用途

  4-アミノサリチル酸（4-アミノサリチルさん）は、結核の治療に使われた抗生物質である。潰瘍性大腸炎やクローン病に強い効果があることが認められ、1940年代から炎症性腸疾患の治療に用いられている。 医薬品としてはカルシウム塩が用いられる。

• 用途

  医薬原料。

• 効能

  抗結核薬

• 化学的特性

  beige powder

• 使用

  antimycobacterial antitubercular;NF-kB inhibitor.
  4-Aminosalicylic acid (p-aminosalicylic acid, PAS), an antituberculosis drug, is a model active pharmaceutical ingredient to study salt and cocrystal formation in a multiple hydrogen-bonding functionality molecule with carboxylic acid, amine, and phenol groups.
  It has also been used as a second line agent to sulfasalazine in people with inflammatory bowel disease such as ulcerative colitis and Crohn's disease.It is typically taken by mouth.

• 定義

  ChEBI: An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.

• 主な応用

  4-Aminosalicylic acid (4-ASA) can be used in the synthesis of:
  Azo derivatives of 4-ASA with anti-inflammatory effects.
  Ammonium 4-aminosalicylate salt polymorphs which are used as pharmaceutical ingredients.
  Salicylic acid-triazole analogs which are used as quorum sensing inhibitors against Pseudomonas aeruginosa.

• 適応症

  p-Aminosalicylic acid is a bacteriostatic that inhibits most tuberculous mycobacteria. In terms of tuberculostatic activity it is inferior to isoniazid and streptomycin. It is nephroand hepatotoxic, and is rarely used. A synonym of this drug is apacizin.

• 一般的な説明

  4-Aminosalicylic acid occurs as a white to yellowish white crystalline solid that darkens on exposure to light or air. It is slightly soluble in water but more soluble in alcohol. Alkali metal salts and the nitric acid salt are soluble in water, but the salts of hydrochloric acid and sulfuric acid are not. The acid undergoes decarboxylation when heated. An aqueous solution has a pH of approximately 3.2. PAS is administered orally in the form of the sodium salt, usually in tablet or capsule form. Symptoms of gastrointestinal irritation are common with both the acid and the sodium salt. Various enteric-coated dosage forms have been used in an attempt to overcome this disadvantage. Other forms that are claimed to improve gastrointestinal tolerance include the calcium salt, the phenyl ester, and a combination with an anion exchange resin (Rezi-PAS). An antacid such as aluminum hydroxide is frequently prescribed. The oral absorption of PAS is rapid and nearly complete, and it is widely distributed into most of the body fluids and tissues, with the exception of the CSF, in which levels are significantly lower.It is excreted primarily in the urine as both unchanged drug and metabolites.

• 生物活性

  4-Aminosalicylic acid is an antimetabolite of p-aminobenzoic acid (PABA) that has antibacterial activity.It is active against streptomycin-sensitive and -resistant strains of M. tuberculosis (MICs = 0.78 and 0.39 μg/ml, respectively), an effect that can be reversed by PABA. 4-Aminosalicylic acid is an alternative substrate for mycobacterial dihydropteroate synthase (FolP1) and misincorporation into the folate pathway leads to accumulation of several folate-dependent metabolites including serine, homocysteine, dUMP, and AICAR, markers of folate pathway inhibition, in a concentration-dependent manner. It reverses manganese-induced increases in rat hippocampal levels of NOD-like receptor protein 3 (NLRP3), cleaved caspase-1, and phosphorylated p65, markers of NLRP3 inflammasome-dependent pyroptosis, when administered at a dose of 300 mg/kg. 4-Aminosalycilic acid is also a building block that has been used in the synthesis of luminescent lanthanide complexes. Formulations containing 4-aminosalicylic acid have been used in the treatment of tuberculosis.

• 作用機序

  p-aminosalicylic acid is thought to act as an antimetabolite interfering with the incorporation of p-aminobenzoic acid into folic acid. When coadministered with INH, PAS is found to reduce the acetylation of INH, itself being the substrate for acetylation, thus increasing the plasma levels of INH. This action may be especially valuable in patients who are rapid acetylators.

• 安全性プロファイル

  Moderately toxic ingestion andother routes. An eye irritant. Mutation data reported.When heated to decomposition it emits toxic fumes ofNOx.

• 代謝

  p-aminosalicylic acid is extensively metabolized by acetylation of the amino group and by conjugation with glucuronic acid and glycine at the carboxyl group. It is used primarily in cases of resistance, retreatment, and intolerance of other agents and is available from the CDC.

• 純化方法

  Crystallise the acid from EtOH. [Beilstein 14 IV 1967.]

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