Mepyramine maleate

Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.

Product Specifications

CAS Number

[59-33-6]

Product Name Alternative

Pyrilamine maleate

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Mepyramine_maleate.html

Purity

99.94

Solubility

DMSO : ≥ 100 mg/mL|H2O : 50 mg/mL (ultrasonic)

Smiles

CN(C)CCN(CC1=CC=C(OC)C=C1)C2=NC=CC=C2.O=C(O)/C=C\C(O)=O

Molecular Formula

C21H27N3O5

Molecular Weight

401.46

Precautions

H302, H315, H319, H335

References & Citations

[1]Hill SJ. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol Rev. 1990 Mar;42 (1) :45-83.|[2]van der Goot H1, et al. Selective ligands as tools to study histamine receptors. Eur J Med Chem. 2000 Jan;35 (1) :5-20.|[3]Fitzsimons CP, et al. Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein. J Biol Chem. 2004 Aug 13;279 (33) :34431-9.|[4]Mojtahedin A, et al. Effects of mepyramine and famotidine on the physostigmine-induced antinociception in the formalin test in rats. Pak J Biol Sci. 2008 Nov 15;11 (22) :2573-8.