(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
- 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。
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靶点
H 3 Receptor
50.3 nM (Kd)
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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.
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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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- 国家：英国
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