Mepyramine maleate

Name: Mepyramine maleate
Brand: tocris
SKU: 0660

Catalog # 0660

Citations (5)

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Key Product Details

Description:	Selective H₁ inverse agonist
Alternative Names:	Pyrilamine maleate
Chemical Name:	2-((2-(Dimethylamino)ethyl)(p-methoxybenzyl)amino)-pyridine maleate
Molecular Weight:	401.46

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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 G_q/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

	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	0.50 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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References

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

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
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

Citations (5)

Showing 1 - 5 of 5 citations Showing All

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Citations are publications that use Bio-Techne 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
Connelly et al. (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol. 157:55
PMID: 19413571
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
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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Mepyramine maleate

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References

Citations (5)

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