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Pyrilamine Maleate Histamine Receptor agonist

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

Cat.No.S4382

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.

Chemical Structure

Molecular Weight: 401.46

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Ciproxifan Maleate Mianserin HCl Astemizole Lafutidine Mizolastine Rupatadine Fumarate Betahistine 2HCl

Chemical Information, Storage & Stability

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

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (199.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 80 mg/mL

Ethanol : 80 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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

%DMSO+ %

Calculation results:

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.

Mechanism of Action

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%.
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. Pyrilamine decreases the number of flinches in a dose dependent manner and decreases c-fos mRNA expression in lumbar spinal cord of rats. Pyrilamine is mainly metabolised 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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8001268/ [2] https://pubmed.ncbi.nlm.nih.gov/10655255/ [3] https://pubmed.ncbi.nlm.nih.gov/12873950/ [4] https://pubmed.ncbi.nlm.nih.gov/2888617/ [5] https://pubmed.ncbi.nlm.nih.gov/3670332/

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