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Mianserin HCl Histamine Receptor antagonist

Name: Mianserin HCl
Brand: Selleck Chemicals
SKU: S1382
Rating: 5 (2 reviews)

Cat.No.S1382

Mianserin (Bolvidon, Norval, Tolvon, ORG GB-94 HCl, Mianserin hydrochloride) is a potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.

Chemical Structure

Molecular Weight: 300.83

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Quality Control

Batch: Purity: 99.88%

99.88

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 Astemizole Lafutidine Mizolastine Rupatadine Fumarate Betahistine 2HCl Levodropropizine

Chemical Information, Storage & Stability

Molecular Weight	300.83	Formula	C₁₈H₂₀N₂·HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	21535-47-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Bolvidon, Norval, Tolvon,ORG GB-94 HCl,Mianserin hydrochloride			Smiles	CN1CCN2C(C1)C3=CC=CC=C3CC4=CC=CC=C42.Cl

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (199.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 30 mg/mL

Ethanol : 21 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.

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

Targets/IC₅₀/Ki	Histamine receptor
In vitro	Mianserin (2 mg/kg s.c.) causes a modest increase of DOPAC levels up to about 30% above base-line, which is statistically significant when compared to saline. Mianserin increases extracellular norepinephnne, but a comparison with desipramine and idazoxan showed that both NE reuptake inhibition and alpha-2 autoreceptor blockade contributed to the mianserin-induced increase in extracellular norepinephnne. Mianserin and eltoprazine displays opposite effects in the elevated plus-maze: Mianserin induces anxiolytic-like effects, while eltoprazine shows anxiogenic-like ones. Mianserin treatment induces a decrease in the number of these sites, while eltoprazine treatment results in an increase.
In vivo	Mianserin, which has a small or no effect in noradrenaline (NA) reuptake but may enhance release by blocking presynaptic inhibition mediated by alpha 2-adrenoceptors, induced regeneration of catecholamine fibers in the rat cerebral cortex. Mianserin attenuates the effects of both m-CPP and SKF 38393 in neonatal 6-OHDA-lesioned rats, suggesting that DA agonist effects are mediated by 5-HT neurochemical systems. Mianserin (10 mg/kg, SC) dose-dependently increases up to about 6 times extracellular dopamine in the medial prefrontal cortex of the rat. Mianserin also dose-dependently increases extracellular noradrenaline in the prefrontal cortex.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8627567/ [2] https://pubmed.ncbi.nlm.nih.gov/7813563/ [3] https://pubmed.ncbi.nlm.nih.gov/1684303/ [4] https://pubmed.ncbi.nlm.nih.gov/7480527/ [5] https://pubmed.ncbi.nlm.nih.gov/8741935/

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