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(R)-(-)-α-Methylhistamine dihydrochloride

CAS No. : 75614-89-0

MCE 站：(R)-(-)-α-Methylhistamine dihydrochloride

产品活性：(R)-(-)-α-Methylhistamine dihydrochloride 是一种有效，选择性和可透过血脑屏障的 H3 组胺受体激动剂，K_d 值为 50.3 nM。(R)-(-)-α-Methylhistamine dihydrochloride 可增强记忆力，减轻大鼠的记忆力障碍。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: (R)-(-)-α-Methylhistamine dihydrochloride is an H3-agonist that is >10 times as potent as histamine (HA). Its selectivity toward H3-receptors is >1000 times as high as that of HA. (R)-(-)-α-Methylhistamine dihydrochloride has only weak affinities for H1 ａnd H2 receptor with a pK_i=4.8 ａnd <3.5, repectively. (R)-(-)-α-Methylhistamine dihydrochloride displays >200-fold selectivity over H4 receptors.

In Vivo: Pretreatment with (R)-(-)-α-Methylhistamine dihydrochloride (RAMH; 10 mg/kg; i.p.; 60 min before training) reverses Propofolinduced (25 mg/kg; i.p.; 30 min before training) memory retention.
(R)-(-)-α-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.

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