Mepyramine maleate_product_DataBase

Bioactivity	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.
Target	Kd: 0.8 nM (Histamine H1 receptor), 5200 nM (Histamine H2 receptor), >3000 nM (Histamine H3 receptor)pKd: 9.4 (Histamine H1 receptor)
Invitro	Mepyramine maleate 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[1], and a pKd of 9.4 for H1 receptor[2]. Mepyramine binds to the H1 receptor with different Kds in Guinea pig brain (0.8 nM), rat brain (9.1 nM) and DDT1-MF-2 and BC3H1 cell (276 nM)[1]. Mepyramine decreases the InsP levels in CHO-gpH1 cells, with log EC50 of -7.94 ± 0.11, and reduces the the maximal response to ATP in CHO-gpH1 cells[3].
In Vivo	Mepyramine obviously decreases the second phase of nociceptive response via i.p at 10 and 20 mg/kg, but shows no significant effect at 5 mg/kg in rats[4].
Name	Mepyramine maleate
CAS	59-33-6
Formula	C21H27N3O5
Molar Mass	401.46
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[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.

PeptideDB

Mepyramine maleate

CAS: 59-33-6 F: C21H27N3O5 W: 401.46