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

CAS No. : 868698-49-1

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

产品活性：(R)-(-)-α-Methylhistamine dihydrobromide 是一种有效的选择性 H3 组胺受体激动剂，K_d 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。

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

作用靶点：Histamine Receptor

In Vitro: (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.

In Vivo: 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.

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