868698-49-1

中文名称 (R)-(-)-α-Methylhistamine dihydrobromide

英文名称 (R)-(-)-α-Methylhistamine dihydrobromide

CAS 868698-49-1

分子式 C6H11N3.2HBr

分子量 206.09

MOL 文件 868698-49-1.mol

868698-49-1 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

(R)()-Α-甲基组胺二盐酸盐

英文别名

(R)-(-)-α-Methylhistamine dihydrobromide
(αR)?-α-?Methyl-1H-?imidazole-?5-?ethanamine Hydrobromide

物理化学性质

储存条件Desiccate at RT

形态白色固体。

水溶解性溶于水至100mM

常见问题列表

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.