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Pyrilamine Maleate

Name: Pyrilamine Maleate
Brand: Selleck Chemicals
SKU: S4382
Rating: 5 (1 reviews)

Synonyms: Mepyramine Maleate

Catalog No.S4382 Purity: 99.96%

Pyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

Pyrilamine Maleate Chemical Structure

CAS: 59-33-6

Selleck's Pyrilamine Maleate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.96%

99.96

Pyrilamine Maleate Related Products

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Signaling Pathway

Histamine Receptor Signaling Pathway

Choose Selective Histamine Receptor Inhibitors

Biological Activity

Description	Pyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

In vitro
In vitro	Pyrilamine blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 of 1.1 μM. Pyrilamine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs and the inward rectifier, IK1 less than 20%. ^[1]

In Vivo
In vivo	Pyrilamine (15 mg/kg/day) significantly decreases the movement time and velocity, as well as the total food consumption and completely abolishes the circadian rhythmicity of locomotion in sham-operated rats. Pyrilamine (15 mg/kg/day) leads to the complete blockade of H(1) receptors in both sham- and portacaval anastomosis-operated rats. ^[2] Pyrilamine decreases the number of flinches in a dose dependent manner and decreases c-fos mRNA expression in lumbar spinal cord of rats. ^[3] Pyrilamine is mainly metabolited into the O-glucuronic acid conjugate of O-demethyl pyrilamine in the rats. The terminal plasma elimination half-life of Pyrilamine does not increase with increasing doses (2.3 hours, 0.7 mg/kg; 1.5 hours, 7.0 mg/kg) and thus pyrilamine does not exhibit dose-dependent elimination. ^[4] Pyrilamine is slightly less mutagenic than Methapyrilene over a comparable range of concentrations, and also induces predominantly small-colony mutants in the L5178Y/TK +/- mouse lymphoma assay. ^[5]

References

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Chemical Information & Solubility

Molecular Weight	401.46	Formula	C₁₇H₂₃N₃O₁.C₄H₄O₄
CAS No.	59-33-6	SDF	Download Pyrilamine Maleate SDF
Smiles	CN(C)CCN(CC1=CC=C(C=C1)OC)C2=CC=CC=N2.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 80 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 80 mg/mL

Ethanol : 80 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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