Catalog Number: 0660
Alternate Names: Pyrilamine maleate
Chemical Name: 2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Storage:
    Store at RT
  • CAS No:
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.
Background References
  1. Mepyramine, a histamine H1 receptor inverse agonist, binds perferentially to a G protein-coupled form of the receptor and sequesters G protein.
    Carlos et al.
    J.Biol.Chem., 2004;279:34431
  2. Distribution, properties and functional characteristics of three classes of histamine receptor.
    Pharmacol.Rev., 1990;42:45
  3. Does the [3H] mepyramine binding site represent the histamine H1 receptor? Re-examination of the histamine H2 receptor with quinine.
    Liu et al.
    J.Pharmacol.Exp.Ther., 1994;268:959

The citations listed below are publications that use Tocris products. Selected citations for Mepyramine maleate include:

1 Citations: Showing 1 - 1

  1. Mast cells are required for experimental oral allergen-induced diarrhea.
    Authors: Brandt Et al.
    J Clin Invest 2003;112:1666

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