生物活性 靶点 体外研究 体内研究
ChemicalBook  CAS数据库列表  (R)-(-)-α-Methylhistamine dihydrobromide

(R)-(-)-α-Methylhistamine dihydrobromide

(R)-(-)-α-Methylhistamine dihydrobromide,868698-49-1,结构式
(R)-(-)-α-Methylhistamine dihydrobromide
  • CAS号:868698-49-1
  • 英文名:(R)-(-)-α-Methylhistamine dihydrobromide
  • 中文名:(R)-(-)-α-Methylhistamine dihydrobromide
  • CBNumber:CB84806424
  • 分子式:C6H12BrN3
  • 分子量:206.09
  • MOL File:868698-49-1.mol
(R)-(-)-α-Methylhistamine dihydrobromide化学性质
  • 储存条件 :Desiccate at RT
  • 形态 :White solid.
  • 水溶解性 :Soluble to 100 mM in water

(R)-(-)-α-Methylhistamine dihydrobromide性质、用途与生产工艺

  • 生物活性 (R)-(-)-α-Methylhistamine dihydrobromide 是一种有效的选择性 H3 组胺受体激动剂,Kd 值为 50.3 nM。(R)-(-)-α-Methylhistamine dihydrobromide 可透过血脑屏障,并可增强记忆力,减轻大鼠的记忆力障碍。
  • 靶点

    H 3 Receptor

    50.3 nM (Kd)

  • 体外研究

    (R)-(-)-α-Methylhistamine dihydrobromide is an H3-agonist that is > 10 times as potent as histamine (HA). Its selectivity toward H3-receptors is > 1,000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrobromide has only weak affinities for H1 and H2 receptor with a pKi=4.8 and < 3.5, repectively. (R)-(-)-α-Methylhistamine dihydrobromide displays >200-fold selectivity over H4 receptors.

  • 体内研究

    Pretreatment with (R)-(-)-α-Methylhistamine dihydrobromide (RAMH; 10 mg/kg; i.p.; 60 min before training) reverses propofol‐induced (25 mg/kg; i.p.; 30 min before training) memory retention.
    (R)-alpha-Methylhistamine dihydrochloride (6.3 mg/kg; i.p.) significantly decreases the steady-state t-MH level in the mouse brain, whereas these compounds produced no significant changes in the HA level.

    Animal Model: Male Sprague‐Dawley rats (10-12 week)
    Dosage: 10 mg/kg
    Administration: IP; 60 min before training
    Result: Reversed propofol‐induced memory retention.
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