Mepyramine maleate

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Cat.No. 0660 - Mepyramine maleate | C17H23N3O.C4H4O4 | CAS No. 59-33-6
Description: Selective H1 inverse agonist
Alternative Names: Pyrilamine maleate
Chemical Name: 2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
Datasheet
Citations (5)
Reviews
Literature

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 40.15 100
DMSO 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 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 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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References

References are publications that support the biological activity of the product.

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 qine J.Pharmacol.Exp.Ther. 268 959 PMID: 8114011


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Keywords: Mepyramine maleate, Mepyramine maleate supplier, Selective, H1, inverse, agonists, Receptors, Histamine, histaminergic, Pyrilamine, maleate, 0660, Tocris Bioscience

5 Citations for Mepyramine maleate

Citations are publications that use Tocris products. Selected citations for Mepyramine maleate include:

Littmann et al (2018) A split luciferase-based probe for quantitative proximal determination of Gαq signalling in live cells. Sci Rep 8 17179 PMID: 30464299

Kurtz et al (2014) Involvement of H1 and H2 receptors and soluble guanylate cyclase in histamine-induced relaxation of rat mesenteric collecting lymphatics. Microcirculation 21 593 PMID: 24702851

Flamand et al (2004) Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP. Br J Pharmacol 141 552 PMID: 14744809

Connelly et al (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157 55 PMID: 19413571

Brandt et al (2003) Mast cells are required for experimental oral allergen-induced diarrhea. J Clin Invest 112 1666 PMID: 14660743


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