2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation MAPK/ERK Pathway Stem Cell/Wnt
  3. Histamine Receptor Opioid Receptor ERK p38 MAPK
  4. Mianserin

Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.

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Mianserin

Mianserin Chemical Structure

CAS No. : 24219-97-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mianserin:

Mianserin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Mianserin

View All Histamine Receptor Isoform Specific Products:

View All Isoforms
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy[1][2][3][4][5].

IC50 & Target[1]

H1 Receptor

 

κ Opioid Receptor/KOR

 

ERK1

 

ERK2

 

In Vitro

Mianserin exhibits 12- and 18-fold higher affinity for human κ-opioid receptors than for μ-opioid receptors and δ-opioid receptors, respectively, with a Ki of 1.7 ± 0.3 μM for κ-opioid receptors[1].
Mianserin selectively activates human κ-opioid receptors in CHO/KOP cells to stimulate [35S]GTPγS binding with an EC50 of 0.53 ± 0.05 μM, with no activity at μ-, δ-opioid receptors, or in untransfected CHO cells[1].
Mianserin (1 μM, 10-120 min) stimulates ERK1/2 phosphorylation in CHO/KOP cells via κ-opioid receptors with an EC50 of 1.5 ± 0.3 μM, peaking at 10 min and remaining elevated for up to 120 min[1].
Mianserin (0.1-30 μM; 15 min) stimulates ERK1/2 phosphorylation in C6 rat glioma cells via endogenous κ-opioid receptors, with an EC50 of 1.6 ± 0.3 μM[1].
Mianserin (1 μM; 10-120 min) stimulates CREB phosphorylation in CHO/KOP cells and C6 rat glioma cells via κ-opioid receptors, with a peak 2-fold increase at 30 min in CHO/KOP cells[1].
Mianserin selectively activates endogenous κ-opioid receptors in rat striatum and nucleus accumbens membranes to stimulate 35S]GTPγS binding, with EC50 values of 0.70 ± 0.05 μM and 0.39 ± 0.06 μM, respectively[1].
Mianserin (10 μM; 10 min) inhibits p38 MAPK and ERK1/2 phosphorylation in primary mouse striatal and hippocampal neurons induced by dynorphin[1].
Mianserin (60 min) potently inhibits specific [3H]octopamine binding to locust Locusta migratoria neuronal octopamine receptors with a Ki of 1.20 ± 0.27 nM[3].
Mianserin inhibits cyclic AMP accumulation mediated by histamine H1 with a Ki of 0.003 μM[5].

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

Mianserin Related Antibodies

Western Blot Analysis[1]

Cell Line: CHO/KOP cells
Concentration: 1 μM
Incubation Time: 10, 30, 60, 90, 120 min
Result: Induced a rapid increase in dual ERK1/2 phosphorylation that peaked at 10 min and remained above control levels for up to 120 min.
Stimulated phosphorylation in a concentration-dependent manner with an EC50 of 1.5 ± 0.3 μM and an Emax corresponding to a 10-fold increase of control values.
Had its stimulatory effect at 1 μM significantly attenuated by 100 nM nor-BNI.
In Vivo

Mianserin (0.12-0.48 μmol/kg; i.p.; single dose) significantly reduces aggressive behavior in male CD1 mice during social encounters in a neutral cage, with minor effects on social and exploratory behaviors in the home cage at 0.48 μmol/kg[2].
Mianserin (0.12-1.92 μmol/kg; p.o.; daily; 12-16 days) administered chronically significantly enhances social investigation in male CD1 mice during social encounters in both home and neutral cages at 0.12 μmol/kg, while 0.12 μmol/kg and 0.48 μmol/kg doses increase digging behavior in the neutral cage[2].
Mianserin (30-40 mg/kg; i.p.; single dose, 30 minutes before testing) increases electroconvulsive threshold and potentiates the anticonvulsant action of select antiepileptics[4].

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

Animal Model: CD1 mice (male, adult, 35-45 g)[2]
Dosage: 0.12 μmol/kg; 0.48 μmol/kg
Administration: I.p.; single dose
Result: Produced no statistically significant effects on behavior categories in the home cage, but increased duration of the social act "nose" and reduced duration of the non-social act "explore" at 0.48 μmol/kg.
Significantly decreased frequency and duration of aggressive behavior, and decreased duration of the social act "attend" in the neutral cage at 0.48 μmol/kg.
Produced no statistically significant effects on behavior categories in either test environment, though reduced duration of the non-social act "explore" in the home cage at 0.12 μmol/kg.
Clinical Trial
Molecular Weight

264.36

Formula

C18H20N2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(CC1)CC2N1C3=CC=CC=C3CC4=CC=CC=C24
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (378.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7827 mL 18.9136 mL 37.8272 mL
5 mM 0.7565 mL 3.7827 mL 7.5654 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1 mg/mL (3.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% Corn Oil

    Solubility: ≥ 1 mg/mL (3.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7827 mL 18.9136 mL 37.8272 mL 94.5680 mL
5 mM 0.7565 mL 3.7827 mL 7.5654 mL 18.9136 mL
10 mM 0.3783 mL 1.8914 mL 3.7827 mL 9.4568 mL
15 mM 0.2522 mL 1.2609 mL 2.5218 mL 6.3045 mL
20 mM 0.1891 mL 0.9457 mL 1.8914 mL 4.7284 mL
25 mM 0.1513 mL 0.7565 mL 1.5131 mL 3.7827 mL
30 mM 0.1261 mL 0.6305 mL 1.2609 mL 3.1523 mL
40 mM 0.0946 mL 0.4728 mL 0.9457 mL 2.3642 mL
50 mM 0.0757 mL 0.3783 mL 0.7565 mL 1.8914 mL
60 mM 0.0630 mL 0.3152 mL 0.6305 mL 1.5761 mL
80 mM 0.0473 mL 0.2364 mL 0.4728 mL 1.1821 mL
100 mM 0.0378 mL 0.1891 mL 0.3783 mL 0.9457 mL
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Mianserin Related Classifications

Help & FAQs
  • 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:

Mianserin24219-97-4MianserineHistamine ReceptorOpioid ReceptorERKp38 MAPKExtracellular signal regulated kinasesCHO/KOP cellsprimary mouse hippocampal neuronsmajor depressionC6 rat glioma cellsERK1/2κ-opioid receptorprimary mouse striatal neuronsLocusta migratoria octopamine receptorCREBInhibitorinhibitorinhibit

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