Mianserin
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.
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- Reinheit: 99.42%
- CAS. Nr.: 24219-97-4
- Formel: C18H20N2
- Molecular Weight:264.36
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Mianserin
MoreAlle Histamine Receptor Isoform-spezifische Produkte anzeigen
MoreAlle Opioid Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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H1 Receptor |
κ Opioid Receptor/KOR |
ERK1 |
ERK2 |
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.
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Cell Line:CHO/KOP cells
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Concentration:1 μM
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Incubation Time:10, 30, 60, 90, 120 min
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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.
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.
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Animal Model:CD1 mice (male, adult, 35-45 g)[2]
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Dosage:0.12 μmol/kg; 0.48 μmol/kg
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Administration:I.p.; single dose
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 24219-97-4
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Appearance Solid
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Molecular Weight 264.36
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Formel C18H20N2
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Color White to off-white
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SMILES
CN(CC1)CC2N1C3=CC=CC=C3CC4=CC=CC=C24
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Synonyms
Mianserine
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
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Most Recent
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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
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (298 KB)
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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)
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Handling Instructions (2659 KB)
Verweise
[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]
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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