アパミン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

• 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。

  P342+P311：呼吸に関する症状が出た場合：医師に連絡すること。

アパミン 価格

アパミン 化学特性,用途語,生産方法

• 解説

  C79H131N31O24S4(2027.36)．アパミン,ハチ毒に含まれる，18個のアミノ酸よりなる塩基性ペプチド．"中枢神経興奮作用をもつ．その主作用は，細胞膜の Ca2＋ 依存性小コンダクタンスの K＋ チャンネルを選択的に抑制するためと考えられている．LD50 58±3 mg/kg(マウス，皮下)．
  森北出版「化学辞典（第2版）

• 化学的特性

  Small, highly potent, highly basic polypeptide.

• 使用

  Apamin has been used:
  
  • As a selective inhibitor of small conductance (SKCa) channels in HEK cells.
  • To inhibit endothelium-derived relaxing factor (EDHF) mediated responses.
  • To block small-conductance Ca₂-activated K current (ISK) in electrophysiological studies in hyperstriatum ventrale, pars caudalis (HVc) neurons.
  
  

• 定義

  Occurs in the venom of the honey bee, Apis mellifera; molecular weight of 2027.38.

• 一般的な説明

  Apamin is a bee venom component and is strongly basic in nature. It has 18 amino acid residues and two disulphide bonds.

• 危険性

  Central nervous system poison able to cross the blood–brain barrier; neurotoxic; poison.

• 安全性プロファイル

  Poison by intravenous, parenteral,intracerebral, and intraperitoneal routes. When heated todecomposition it emits toxic fumes of SOx and NOx.

• 酵素阻害剤

  This bee venom octadecapeptide toxin (FW = 2027.34 g/mol; CAS 24345- 16-2; NCBI Reference Sequence: NP_001011612.1) potently blocks the small-conductance Ca 2+ -activated potassium ion (or SK) channels hSK1 as well as rSK2, with IC50 values of 3.3 nM and 83 pM. It shows greater effectiveness at the SK2 channel (IC50 = 0.06-0.4 nM) than SK1 (IC50 = 1- 12 nM). SK3 (IC50 = 1-13 nM), and SK4 (IC50 = 1 μM) channels, and is active against channels within neurons, vascular endothelium, bladder smooth muscle, and certain cancers. Apamin does not inhibit human cardiac Na + current, L-type Ca 2+ current or other major K+ currents. Structurally, apamin forms a stable structure, consisting of a C-terminal a- helix and two reverse turns, that is stabilized by two disulfide bonds connecting Cys-1 to Cys-11 and Cys-3 to Cys-15. A minor constituent of venom of the bee (Apis mellifera), apamin amounts to only 2-3% (w/w) of its dry venom. The smallest known neurotoxic polypeptide, apamin is derived by proteolytic processing of the 48-residue pre-pro-protein. The precursors of the bee venom constituents apamin and MCD peptide are encoded by two genes in tandem which share the same 3'-exon.

アパミン 生産企業

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24345-16-2, アパミン キーワード