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

Mianserin hydrochloride  (Synonyms: Org GB 94)

Cat. No.: HY-B0188A Purity: 99.95%
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Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.

For research use only. We do not sell to patients.

Mianserin hydrochloride

Mianserin hydrochloride Chemical Structure

CAS No. : 21535-47-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Mianserin hydrochloride:

Mianserin hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Mianserin hydrochloride

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 hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy[1][2][3][4][5].

IC50 & Target[5]

H1 Receptor

 

κ Opioid Receptor/KOR

 

ERK1

 

ERK2

 

In Vitro

Mianserin hydrochloride 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 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride 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 hydrochloride (10 μM; 10 min) inhibits p38 MAPK and ERK1/2 phosphorylation in primary mouse striatal and hippocampal neurons induced by dynorphin[1].
Mianserin hydrochloride (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 hydrochloride 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 hydrochloride Related Antibodies

Cell Viability AssayCHO/KOP cells

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 hydrochloride (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 hydrochloride (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 hydrochloride (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.
Molecular Weight

300.83

Formula

C18H21ClN2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CN(CC1)CC2N1C3=CC=CC=C3CC4=CC=CC=C24.Cl
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (166.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (83.10 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3241 mL 16.6207 mL 33.2414 mL
5 mM 0.6648 mL 3.3241 mL 6.6483 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • 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

Concentration (start)

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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: ≥ 2.5 mg/mL (8.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.95%

SDS (393 KB)

COA (258 KB) HNMR (250 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.3241 mL 16.6207 mL 33.2414 mL 83.1034 mL
5 mM 0.6648 mL 3.3241 mL 6.6483 mL 16.6207 mL
10 mM 0.3324 mL 1.6621 mL 3.3241 mL 8.3103 mL
15 mM 0.2216 mL 1.1080 mL 2.2161 mL 5.5402 mL
20 mM 0.1662 mL 0.8310 mL 1.6621 mL 4.1552 mL
25 mM 0.1330 mL 0.6648 mL 1.3297 mL 3.3241 mL
30 mM 0.1108 mL 0.5540 mL 1.1080 mL 2.7701 mL
40 mM 0.0831 mL 0.4155 mL 0.8310 mL 2.0776 mL
50 mM 0.0665 mL 0.3324 mL 0.6648 mL 1.6621 mL
60 mM 0.0554 mL 0.2770 mL 0.5540 mL 1.3851 mL
80 mM 0.0416 mL 0.2078 mL 0.4155 mL 1.0388 mL
DMSO 100 mM 0.0332 mL 0.1662 mL 0.3324 mL 0.8310 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mianserin hydrochloride Related Classifications

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  • 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:

Mianserin21535-47-7Org GB 94Org GB94Org GB-94Histamine ReceptorOpioid ReceptorERKp38 MAPKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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