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Submit Review(R)-(-)-α-Methylhistamine dihydrobromide
Discontinued Product
0569 has been discontinued.
View all Histamine H<sub>3</sub> Receptors products.
说明： Potent, standard H3 agonist
化学名： (R)-(-)-α-Methyl-1H-imidazole-4-ethanamine dihydrobromide
纯度： ≥98% (HPLC)
生物活性
(R)-(-)-α-Methylhistamine dihydrobromide is a very potent, high affinity H3 agonist (KD = 50.3 nM) that displays > 200-fold selectivity over H4 receptors. Inhibits H3-mediated histamine synthesis and release in the CNS and stimulates H4-mediated eosinophil shape change (EC50 = 66 nM).
S-enantiomer also available.
技术数据
| 分子量 | 287 |
| 公式 | C6H11N3.2HBr |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 868698-49-1 |
| PubChem ID | 45037031 |
| InChI Key | RWHNAAABSGVRDT-ZJIMSODOSA-N |
| Smiles | N[C@H](C)CC1=CNC=N1.Br.Br |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书
参考文献
参考文献是支持产品生物活性的出版物。
Buckland et al (2003) Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor. Br.J.Pharmacol. 140 1117 PMID: 14530216
Hew et al (1990) Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands. Br.J.Pharmacol. 101 621 PMID: 1963802
Oishi et al (1989) Effects of histamine H3-agonist (R)-α-methylhistamine and the antagonist thioperamide on histamine modulation in the mouse and rat brain. J.Neurochem. 52 1388 PMID: 2540269
Schwartz et al (1990) A third histamine receptor subtype - characterization, localization and functions of the H3-receptor. Agents Actions 30 13 PMID: 1695431
Shahid et al (2009) Histamine, histamine receptors, and their role in immunomodulation: An updated systematic review. Open Immunol.J. 2 9
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关键词: (R)-(-)-alpha-Methylhistamine dihydrobromide, (R)-(-)-alpha-Methylhistamine dihydrobromide supplier, Potent, H3, agonists, Receptors, Histamine, histaminergic, (R)-(-)-alpha-Methylhistamine, dihydrobromide, 0569, Tocris Bioscience
4 篇 (R)-(-)-α-Methylhistamine dihydrobromide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 (R)-(-)-α-Methylhistamine dihydrobromide 的部分引用包括：
Kim et al (2013) Effects of histamine on cultured interstitial cells of cajal in murine small intestine. Korean J Physiol Pharmacol 17 149 PMID: 23626477
Spaethling et al (2014) Serotonergic neuron regulation informed by in vivo single-cell transcriptomics. J Clin Invest 28 771 PMID: 24192459
Rapanelli et al (2016) The Histamine H3 Receptor Differentially Modulates Mitogen-activated Protein Kinase (MAPK) and Akt Signaling in Striatonigral and Striatopallidal Neurons. J Biol Chem. 291 21042 PMID: 27510032
Holden et al (2007) Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells. FASEB J 152 891 PMID: 17891168
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该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.
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