Chemical Name: 2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective inverse agonist for the H1 receptor. Inhibits histamine induced inositol phosphate (InsP) production (log EC50 = -7.94) and intracellular calcium mobilization. Sequesters Gq/11 protein, reducing its availability for other receptors associated with the same signaling pathway.
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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
phosphate buffered saline
40.15
100
DMSO
40.15
100
water
40.15
100
Preparing Stock Solutions
The following data is based on the product molecular weight 401.46. Batch specific molecular weights may vary from batch to batch due to solvent 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
2.49 mL
12.45 mL
24.91 mL
5 mM
0.5 mL
2.49 mL
4.98 mL
10 mM
0.25 mL
1.25 mL
2.49 mL
50 mM
0.05 mL
0.25 mL
0.5 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Carloset al (2004) Mepyramine, a histamine H1 receptor inverse agonist, binds perferentially to a G protein-coupled form of the receptor and sequesters G protein. J.Biol.Chem. 279 34431 PMID: 15192105
Hill
(1990) Distribution, properties and functional characteristics of three classes of histamine receptor. Pharmacol.Rev. 42 45 PMID: 2164693
Liuet al (1994) Does the [3H] mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H2 receptor with quinine. J.Pharmacol.Exp.Ther. 268 959 PMID: 8114011