Mepyramine maleate (Synonyms: Pyrilamine maleate)

Name: Mepyramine maleate
Brand: MedChemExpress
SKU: HY-B1281
Rating: 5.0 (2 reviews)

Cat. No.: HY-B1281 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

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

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Mepyramine maleate Chemical Structure

CAS No. : 59-33-6

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10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

Other Forms of Mepyramine maleate:

Mepyramine maleate (Standard) Get quote

2 Publications Citing Use of MCE Mepyramine maleate

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

H₁ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	3.3 nM Compound: pyrilamine	Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs	[PMID: 23403082]
HEK293	IC₅₀	1.4 nM Compound: Pyrilamine	Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method	[PMID: 27876250]
HEK293	IC₅₀	1.9 nM Compound: Pyrilamine	Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting	[PMID: 27997171]
RBL-2H3	IC₅₀	0.0815 μM Compound: 5i	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method	[PMID: 31703894]
RBL-2H3	IC₅₀	0.0926 μM Compound: 5i	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr	[PMID: 31703894]
RBL-2H3	IC₅₀	0.132 μM Compound: 5i	Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety	[PMID: 31703894]

In Vitro

Mepyramine maleate is an antagonist of histamine H1 receptor, with K_ds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively^[1], and a pK_d of 9.4 for H1 receptor^[2]. Mepyramine binds to the H1 receptor with different K_ds 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].

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

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].

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

Molecular Weight

401.46

Formula

C₂₁H₂₇N₃O₅

CAS No.

59-33-6

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

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)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (249.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (124.55 mM; Need ultrasonic)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (249.09 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (253 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Hill SJ. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol Rev. 1990 Mar;42(1):45-83. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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	[1]. Hill SJ. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol Rev. 1990 Mar;42(1):45-83. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.4909 mL	12.4545 mL	24.9091 mL	62.2727 mL
	5 mM	0.4982 mL	2.4909 mL	4.9818 mL	12.4545 mL
	10 mM	0.2491 mL	1.2455 mL	2.4909 mL	6.2273 mL
	15 mM	0.1661 mL	0.8303 mL	1.6606 mL	4.1515 mL
	20 mM	0.1245 mL	0.6227 mL	1.2455 mL	3.1136 mL
	25 mM	0.0996 mL	0.4982 mL	0.9964 mL	2.4909 mL
	30 mM	0.0830 mL	0.4152 mL	0.8303 mL	2.0758 mL
	40 mM	0.0623 mL	0.3114 mL	0.6227 mL	1.5568 mL
	50 mM	0.0498 mL	0.2491 mL	0.4982 mL	1.2455 mL
	60 mM	0.0415 mL	0.2076 mL	0.4152 mL	1.0379 mL
	80 mM	0.0311 mL	0.1557 mL	0.3114 mL	0.7784 mL
	100 mM	0.0249 mL	0.1245 mL	0.2491 mL	0.6227 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Mepyramine maleate Related Classifications

Neurological Disease Endocrinology

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mepyramine59-33-6PyrilamineHistamine ReceptorInhibitorinhibitorinhibit

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Mepyramine maleate (Synonyms: Pyrilamine maleate)

Customer Review

Other Forms of Mepyramine maleate:

Mepyramine maleate Related Antibodies

2 Publications Citing Use of MCE Mepyramine maleate

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Mepyramine maleate Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Mepyramine maleate Related Classifications

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