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(R)-(-)-α-Methylhistamine dihydrobromide

Catalog #: 0569
4 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
0569/10
0569/50
(R)-(-)-α-Methylhistamine dihydrobromide | CAS No. 868698-49-1 | Histamine H3 Receptor Agonists
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Description: Potent, standard H3 agonist

Chemical Name: (R)-(-)-α-Methyl-1H-imidazole-4-ethanamine dihydrobromide

Purity: ≥98%

Product Details
Citations (4)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

(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.

Technical Data

M.Wt:
287
Formula:
C6H11N3.2HBr
Solubility:
Soluble to 100 mM in water
Purity:
≥98%
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  3. Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor.
    Buckland et al.
    Br.J.Pharmacol., 2003;140:1117
  4. Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands.
    Hew et al.
    Br.J.Pharmacol., 1990;101:621
  5. 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
  6. A third histamine receptor subtype - characterization, localization and functions of the H3-receptor.
    Schwartz et al.
    Agents Actions, 1990;30:13
  7. Histamine, histamine receptors, and their role in immunomodulation: An updated systematic review.
    Shahid et al.
    Open Immunol.J., 2009;2:9

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Citations for (R)-(-)-α-Methylhistamine dihydrobromide

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

4 Citations: Showing 1 - 4

  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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