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Mianserin HCl Histamine Receptor antagonist

Cat.No.S1382

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

Chemical Structure

Molecular Weight: 300.83

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 300.83 Formula

C18H20N2·HCl

Storage (From the date of receipt)
CAS No. 21535-47-7 Download SDF Storage of Stock Solutions

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

In vivo
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In vivo Formulation Calculator (Clear solution)

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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.

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Mechanism of Action

Targets/IC50/Ki
Histamine receptor [1]
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. [1] 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. [2]

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. [3] 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. [4] 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. [5]

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7480527/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8741935/

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