Catalog Number: 0569
Chemical Name: (R)-(-)-α-Methyl-1H-imidazole-4-ethanamine dihydrobromide
Biological Activity
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).

Available as part of the Histamine H3 Receptor Tocriset™. S-enantiomer also available.

Technical Data
  • M.Wt:
    287
  • Formula:
    C6H11N3.2HBr
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    868698-49-1
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.
Additional Information
Other Product-Specific Information:
Background References
  1. Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor.
    Buckland et al.
    Br.J.Pharmacol., 2003;140:1117
  2. Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands.
    Hew et al.
    Br.J.Pharmacol., 1990;101:621
  3. Effects of histamine H3-agonist (R)-α-methylhistamine and the antagonist thioperamide on histamine modulation in the mouse and rat brain.
    Oishi et al.
    J.Neurochem., 1989;52:1388
  4. Synthesis of S-[3-(4(5)-imidazolyl)propyl]-N-[2-(4-[125I]-iodophenylethyl]isothiourea sulfate [125I]-iodophenpropit), a new probe for histamine H3 receptor binding sites.
    Menge et al.
    J.Labelled Comp.Radiopharm. XXXI, 1992;10:781
  5. A third histamine receptor subtype - characterization, localization and functions of the H3-receptor.
    Schwartz et al.
    Agents Actions, 1990;30:13
Citations:

The citations listed below are publications that use Tocris products. Selected citations for (R)-(-)-α-Methylhistamine dihydrobromide include:

4 Citations: Showing 1 - 4
Filter your results:

  1. The Histamine H3 Receptor Differentially Modulates Mitogen-activated Protein Kinase (MAPK) and Akt Signaling in Striatonigral and Striatopallidal Neurons.
    Authors: Rapanelli Et al.
    J Biol Chem. 2016;291:21042
  2. Serotonergic neuron regulation informed by in vivo single-cell transcriptomics.
    Authors: Spaethling Et al.
    J Clin Invest 2014;28:771
  3. Effects of histamine on cultured interstitial cells of cajal in murine small intestine.
    Authors: Kim Et al.
    Korean J Physiol Pharmacol 2013;17:149
  4. Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells.
    Authors: Holden Et al.
    FASEB J 2007;152:891

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