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(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
英文别名:
(R)-(-)-α-Methylhistamine dihydrobromide;(αR)?-α-?Methyl-1H-?imidazole-?5-?ethanamine Hydrobromide;(R)()αMethylhistamine dihydrobromide,(R) ( ) α Methylhistamine dihydrobromide
中文名:
(R)-(-)-α-Methylhistamine dihydrobromide
中文别名:
化合物 T12630;(R)()-Α-甲基组胺 二盐酸盐
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
安全信息

(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.

(R)-(-)-α-Methylhistamine dihydrobromide 上下游产品信息

上游原料

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(R)-(-)-α-Methylhistamine dihydrobromide 生产厂家

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868698-49-1, (R)-(-)-α-Methylhistamine dihydrobromide 相关搜索:

  • 化合物 T12630
  • (R)()-Α-甲基组胺 二盐酸盐
  • 868698-49-1
  • (R)()αMethylhistamine dihydrobromide,(R) ( ) α Methylhistamine dihydrobromide
  • (αR)?-α-?Methyl-1H-?imidazole-?5-?ethanamine Hydrobromide
  • (R)-(-)-α-Methylhistamine dihydrobromide
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