Cat. No. 0569
Chemical Name: (R)-(-)-α-Methyl-1H-imidazole-4-etha
Biological ActivityVery 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). Part of the Histamine H3 Receptor Tocriset™. (S)-(+)-α-Methylhistamine dihydrobromide (Cat. No. 0572) also available.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Shahid et al (2009) Histamine, histamine receptors, and their role in immunomodulation: An updated systematic review. Open Immunol.J. 2 9.
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.
Schwartz et al (1990) A third histamine receptor subtype - characterization, localization and functions of the H3-receptor. Agents Actions 30 13. PMID: 1695431.
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.
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Citations are publications that use Tocris products. Selected citations for (R)-(-)-α-Methylhistamine dihydrobromide include:
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 .
Spaethling et al (2014) Serotonergic neuron regulation informed by in vivo single-cell transcriptomics. J Clin Invest 28 771. PMID: 24192459.
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.
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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Keywords: (R)-(-)-a-Methylhistamine dihydrobromide, supplier, Potent, H3, agonists, Receptors, Histamine, histaminergic, (R)-(-)-alpha-Methylhistamine, dihydrobromide, Tocris Bioscience, Histamine H3 Receptor Agonist products