| 中文名称 |
(R)-(-)-α-Methylhistamine dihydrochloride
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| 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
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| 英文名称 |
(R)-(-)-α-Methylhistamine dihydrochloride
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| 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
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| Cas No. |
75614-89-0
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| 分子式 |
C6H11N3.2[HCl]
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| 分子量 |
198.09
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| 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)
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| 详情描述 |
(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。
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| 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。
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| 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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
H3 Receptor 50.3 nM (Kd)
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| 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.
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| 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.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| 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)-
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| 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]. 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)-
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。