Cat. No.: HY-B0188

Mianserin

(Synonyms: Mianserine)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

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

Purity: 99.42%
CAS No.: 24219-97-4
Formula: C₁₈H₂₀N₂
Molecular Weight:264.36

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Mianserin Chemical Structure

CAS No.: 24219-97-4

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

Biological Activity

Description

IC₅₀ & Target^[1]

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 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 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 K_i of 1.20 ± 0.27 nM^[3].
Mianserin 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.

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 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 (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 24219-97-4
Appearance Solid
Molecular Weight 264.36
Formula C₁₈H₂₀N₂
Color White to off-white
SMILES

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

Mianserine
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

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

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

3.7827 mL

18.9136 mL

37.8272 mL

5 mM

0.7565 mL

3.7827 mL

7.5654 mL

10 mM

0.3783 mL

1.8914 mL

3.7827 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, 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.

Molarity Calculator

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

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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: ≥ 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.

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:

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (298 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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

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

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Publications Citing Use of MedChemExpress (MCE) Mianserin

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 Related Classifications

HY-B0188 Related Classifications