1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor

Mepyramine maleate (Synonyms: Pyrilamine maleate)

Cat. No.: HY-B1281 Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Mepyramine maleate Chemical Structure

Mepyramine maleate Chemical Structure

CAS No. : 59-33-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

Kd: 0.8 nM (Histamine H1 receptor), 5200 nM (Histamine H2 receptor), >3000 nM (Histamine H3 receptor)[1]
pKd: 9.4 (Histamine H1 receptor)[2]

In Vitro

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (373.64 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4909 mL 12.4545 mL 24.9091 mL
5 mM 0.4982 mL 2.4909 mL 4.9818 mL
10 mM 0.2491 mL 1.2455 mL 2.4909 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

Briefly, cells are seeded in 24-well cluster dishes and cultured for 24 h (70-80% confluence) in DMEM. Cells are then washed, and the medium is replaced for DMEM without calf serum plus the addition of myo-[3H]inositol (2 μCi/mL) and cultured for 24 h. Thereafter, the medium is aspirated and replaced with DMEM without calf serum containing 10 mM LiCl and incubated for 20 min. Cells are then stimulated for 20 min with histamine in concentrations ranging from 1 nM to 100 μM in a final volume of 300 μL in the presence or absence of [3H]inositol the concentrations indicated in each particular experiment. The incubation is stopped by the addition of 900 μL of cold chloroform, methanol, 0.12 M HCl (1:2:1 v/v, freshly prepared), and phases are split by the addition of 300 μL of water and 300 μL of chloroform. The mixture is then centrifuged at 1500 × g for 10 min, and the total water-soluble inositol phosphate fraction is purified by anion exchange chromatography. Radioactivity of the eluted fractions is measured using a liquid scintillation counter. Results are expressed as the ratio obtained when total [3H]inositol phosphate radioactivity is normalized to total [3H]inositol radioactivity recovered from the initial water wash of the columns[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rats[4]
Healthy adult male albino Wistar rats weighing 200-220 g are maintained in polypropylene cages with 6 rats in each cage with food and water available ad libitum. Mepyramine is dissolved in normal saine. Mepyramine at doses of 5, 10, and 20 mg/kg and intraperitoneally injected 30 min before induction of nociception. Physostigmine at doses of 0.05, 0.1, and 0.2 mg/kg, and atropine at a dose of 2 mg/kg, are subcutaneously administered 20 and 40 min before induction of formalin-induced pain, respectively. Atropine (2 mg/kg, s.c.) is injected 20 min before subcutaneous injection of physostigmine (0.1 mg/kg). In combined treatment, intraperitoneal injections of mepyramine (10 mg/kg) and famotidine (20 mg/kg) are performed 10 min before physostigmine (0.1 mg/kg, s.c.) and 10 min after atropine (0.2 mg/kg, s.c.) administrations. Drug solutions are intraperitoneally injected in a volum of 1 mL/kg, using a 25-gauge injection needle. Subcutaneous injections of drug solutions are perfoemed in a constant volume 0.2 mL per rat at the neck region using a 27-gauge injection needle[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

401.46

Formula

C₂₁H₂₇N₃O₅

CAS No.

59-33-6

SMILES

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

Storage

4°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Mepyramine maleate
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HY-B1281
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Mepyramine maleate

Cat. No.: HY-B1281