(R)-(-)-α-Methylhistamine dihydrochloride (Synonyms: (R)-(-)-α-甲基组胺二盐酸盐)
目录号: PL14956 纯度: ≥99%
CAS No. :75614-89-0
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中文名称
(R)-(-)-α-Methylhistamine dihydrochloride
中文别名
( - )-α-甲基胺盐酸盐;(-)-Α-甲基胺盐酸盐;(2R)-1-(1H-咪唑-4-基)-2-丙胺二盐酸盐;双联邻苯二酚硼酸酯;R(-)-Alpha-甲基组胺二盐酸;(-)-Alpha-甲基胺盐酸盐
英文名称
(R)-(-)-α-Methylhistamine dihydrochloride
英文别名
1H-Imidazole-5-ethanamine,a-methyl-, hydrochloride (1:2), (aR)-;R(-)-α-Methyl Histamine Dihydrochloride;R(-)-A-METHYLHISTAMINE DIHYDROCHLORIDE;R(-)-α-Methyl Histam;(R)(−)-α-Methyl-1H-imidazole-4-ethanamine dihydrochloride;(R)-2-(1H-Imidazol-4-yl)-1-methyl-ethylamine dihydrochloride;(R)-(-)-α-Methylhistamine dihydrochloride
Cas No.
75614-89-0
分子式
C6H11N3.2[HCl]
分子量
198.09
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
(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。
生物活性
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.
性状
Solid
IC50 & Target[1][2]
H3 Receptor 50.3 nM (Kd)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Pretreatment with (R)-(-)-α-Methylhistamine dihydrochloride (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)-(-)-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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Arrang JM, et al. Highly potent and selective ligands for histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.
[2]. Mohammad Shahid, et al. Histamine, Histamine Receptors, and their Role in Immunomodulation: An Updated Systematic Review. The Open Immunology Journal, 2009, 2, 9-41.
[3]. Oishi R, et al. Effects of the histamine H3-agonist (R)-
溶解度数据
In Vitro: DMSO : 250 mg/mL (1262.05 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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