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(R)-(-)-α-Methylhistamine dihydrochloride
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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,Kd 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 pKi=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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