Chemical Name: (R)-(-)-α-Methyl-1H-imidazole-4-ethanamine dihydrobromide
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.
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.
Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
Tollefson and Taylor
CNS Drug Reviews, 2000;6:303
Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor.
Buckland et al.
Characterization of histamine-H3 receptors in guinea pig ileum with H3-selective ligands.
Hew et al.
Effects of histamine H3-agonist (R)-α-methylhistamine and the antagonist thioperamide on histamine modulation in the mouse and rat brain.
Oishi et al.
A third histamine receptor subtype - characterization, localization and functions of the H3-receptor.
Schwartz et al.
Agents Actions, 1990;30:13
Histamine, histamine receptors, and their role in immunomodulation: An updated systematic review.
Shahid et al.
Open Immunol.J., 2009;2:9
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
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
Serotonergic neuron regulation informed by in vivo single-cell transcriptomics.
Authors: Spaethling Et al.
J Clin Invest 2014;28:771
Effects of histamine on cultured interstitial cells of cajal in murine small intestine.
Authors: Kim Et al.
Korean J Physiol Pharmacol 2013;17:149
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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