Cat. No.: HY-B0188A

Mianserin hydrochloride

(Synonyms: Org GB 94)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 99.95%
CAS No.: 21535-47-7
Formula: C₁₈H₂₁ClN₂
Molecular Weight:300.83

Storage:

4°C, sealed storage, away from moisture

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

Mianserin hydrochloride Chemical Structure

CAS No.: 21535-47-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[5]

H₁ Receptor

κ Opioid Receptor/KOR

ERK1

ERK2

All Histamine Receptor Isoforms :

All Opioid Receptor Isoforms :

All ERK Isoforms :

All p38 MAPK Isoforms :

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 K_i 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 K_i of 1.20 ± 0.27 nM^[3].
Mianserin hydrochloride inhibits cyclic AMP accumulation mediated by histamine H1 with a K_i of 0.003 μM^[5].

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

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 E_max 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.

Chemical Information

CAS No. 21535-47-7
Appearance Solid
Molecular Weight 300.83
Formula C₁₈H₂₁ClN₂
Color White to light yellow
SMILES

CN(CC1)CC2N1C3=CC=CC=C3CC4=CC=CC=C24.Cl
Synonyms

Org GB 94
Structure Classification
- Alkaloids
- Other Alkaloids
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)

Publications (1)

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Journal Impact Factor

Insect Biochem Mol Biol

Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]

2025 May:180:104312. PMID: 40245998

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3241 mL

16.6207 mL

33.2414 mL

5 mM

0.6648 mL

3.3241 mL

6.6483 mL

10 mM

0.3324 mL

1.6621 mL

3.3241 mL

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

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

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Olianas MC, et al. The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors. Br J Pharmacol. 2012;167(6):1329-1341. [Content Brief]

[2]. Gao B, et al. Effects of acute and chronic administration of the antidepressants, imipramine, phenelzine and mianserin, on the social behaviour of mice. Neuropharmacology. 1994;33(6):813-824. [Content Brief]

[3]. Roeder T. High-affinity antagonists of the locust neuronal octopamine receptor. Eur J Pharmacol. 1990 Nov 27;191(2):221-4. [Content Brief]

[4]. Borowicz KK, et al. Acute and chronic treatment with mianserin differentially affects the anticonvulsant activity of conventional antiepileptic drugs in the mouse maximal electroshock model. Psychopharmacology (Berl). 2007;195(2):167-174. [Content Brief]

[5]. Nowak J Z, Arrang J M, Schwartz J C, et al. Interaction between mianserin, an antidepressant drug, and central H1-and H2-histamine-receptors: in vitro and in vivo studies and radioreceptor assay[J]. Neuropharmacology, 1983, 22(3): 259-266.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Mianserin hydrochloride

1 Cited Publications

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Mianserin hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Mianserin hydrochloride

All Histamine Receptor Isoforms

All Opioid Receptor Isoforms

All ERK Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Mianserin hydrochloride Related Classifications

HY-B0188A Related Classifications