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High affinity H3 receptor antagonist (Ki = 43.8 nM). Displays selectivity against H1 and H2 receptors (IC50 >10 μM). Increases the release of histamine in the cerebral cortex. Displays no activity at histamine methyltransferase in vitro at concentrations up to 3 μM. Brain penetrant.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 317.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.15 mL||15.75 mL||31.5 mL|
|5 mM||0.63 mL||3.15 mL||6.3 mL|
|10 mM||0.31 mL||1.57 mL||3.15 mL|
|50 mM||0.06 mL||0.31 mL||0.63 mL|
References are publications that support the biological activity of the product.
Tedford et al (1995) Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. J.Pharmacol.Exp.Ther. 275 598 PMID: 7473144
Tedford et al (1999) Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1160 PMID: 10215700
Yates et al (1999) Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1151 PMID: 10215699
If you know of a relevant reference for GT 2016, please let us know.
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Keywords: GT 2016, GT 2016 supplier, GT2016, histamine, h3, antagonists, histaminergic, selective, brain, penetrant, centrally, active, Histamine, H3, Receptors, 2419, Tocris Bioscience
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.