Mepyramine maleate is a selective inverse agonist for the H₁ receptor. Inhibits histamine induced inositol phosphate (InsP) production (log EC₅₀ = -7.94) and intracellular calcium mobilization. Sequesters G_q/11 protein, reducing its availability for other receptors associated with the same signaling pathway.

Product Specifications

Molecular Weight

401.46

Formula

C₁₇H₂₃N₃O.C₄H₄O₄

Storage

Store at RT

Chemical Name

2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate

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.

Solubility

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

Preparing Stock Solutions for Mepyramine maleate

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 all 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	0.50 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	0.50 mL

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Background References

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

Hill Distribution, properties and functional characteristics of three classes of histamine receptor. Pharmacol.Rev. 1990 PMID: 2164693
Liu Does the [³H] mepyramine binding site represent the histamine H₁ receptor? Re-examination of the histamine H₂ receptor with qine J.Pharmacol.Exp.Ther. 1994 PMID: 8114011
Carlos 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. 2004 PMID: 15192105

Mepyramine maleate

Tocris Bioscience, part of Bio-Techne | Catalog # 0660

Key Product Details

Description

Alternative Names

View all Histamine H1 Inverse Agonists »

Product Description