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 | 401.46 |
| Formula | C17H23N3O.C4H4O4 |
| Storage | Store at RT |
| CAS Number | 59-33-6 |
| PubChem ID | 5284451 |
| InChI Key | JXYWFNAQESKDNC-BTJKTKAUSA-N |
| Smiles | OC(=O)C=C/C(O)=O.COC1=CC=C(CN(CCN(C)C)C2=CC=CC=N2)C=C1 |
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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Carlos et 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
Liu et 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
Keywords: Mepyramine maleate, supplier, Selective, H1, inverse, agonists, Receptors, Histamine, histaminergic, Pyrilamine, maleate, Histamine, H1, Receptors, Histamine, H1, Receptors, Tocris Bioscience
