Mianserin HCl (ORG GB-94 HCl)

Alias: ORG GB-94 HCl; Mianserin; Depnon; Lerivon; Lumin; Lantanon; ORG GB-94 HCl; ORG GB 94 HCl; Norval; Tolvon
Cat No.:V1210 Purity: ≥98%
Mianserin HCl (formerly ORG GB-94; ORG-GB 94; Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon), the hydrochloride salt of mianserin which is a psychoactive tetracyclic compound, is a novel and potent antagonist (inverse agonist) of H1 histamine receptor and 5-HT serotonin receptors used for the treatment of depression.
Mianserin HCl (ORG GB-94 HCl) Chemical Structure CAS No.: 21535-47-7
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Mianserin HCl (ORG GB-94 HCl):

  • Mianserin (ORG GB-94)
  • Mianserin-d3 hydrochloride (Org GB 94-d3)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Mianserin HCl (formerly ORG GB-94; ORG-GB 94; Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon), the hydrochloride salt of mianserin which is a psychoactive tetracyclic compound, is a novel and potent antagonist (inverse agonist) of H1 histamine receptor and 5-HT serotonin receptors used for the treatment of depression. Hematological issues as well as sleepiness could result from it. Though its exact mode of action is unknown, it appears to block certain types of serotonin, histamine H1, and alpha-adrenergic receptors.

Biological Activity I Assay Protocols (From Reference)
Targets
H1 Receptor
ln Vitro

In vitro activity: Mianserin (2 mg/kg s.c.) produces a statistically significant increase in DOPAC levels from a modest baseline to approximately 30% above baseline when compared to saline. Mianserin causes an increase in extracellular norepinephne; however, when compared to desipramine and idazoxan, it was found that the increase in extracellular norepinephne was caused by both NE reuptake inhibition and alpha-2 autoreceptor blockade.[1] Mianserin and eltoprazine exhibit opposing effects in the elevated plus-maze: Eltoprazine exhibits anxiogenic effects whereas menaserin induces anxiolytic effects. Treatment with miranserin causes these sites to become fewer in number, whereas treatment with eltoprazine causes them to become more numerous.[2]

ln Vivo
Mianserin induced regeneration of catecholamine fibers in the rat cerebral cortex. Mianserin has little to no effect on noradrenaline (NA) reuptake, but it may enhance release by blocking presynaptic inhibition mediated by alpha 2-adrenoceptors. In neonatal 6-OHDA-lesioned rats, mianserin attenuates the effects of both m-CPP and SKF 38393, indicating that the actions of DA agonists are mediated by 5-HT neurochemical systems.[4] Mianserin (10 mg/kg, SC) increases extracellular dopamine in the rat's medial prefrontal cortex in a dose-dependent manner up to a factor of approximately six. In the prefrontal cortex, meserin also raises extracellular noradrenaline in a dose-dependent manner.[5]
Animal Protocol
10 mg/kg, SC
Rats
References

[1]. J Pharmacol Exp Ther . 1996 May;277(2):852-60.

[2]. Eur J Pharmacol . 1994 Sep 1;262(1-2):125-31.

[3]. Neuroreport . 1991 Sep;2(9):525-8.

[4]. Psychopharmacology (Berl) . 1995 Jun;119(4):466-73.

[5]. Psychopharmacology (Berl) . 1996 Jan;123(2):127-30.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H21CLN2
Molecular Weight
300.83
Exact Mass
300.14
Elemental Analysis
C, 71.87; H, 7.04; Cl, 11.78; N, 9.31
CAS #
21535-47-7
Related CAS #
Mianserin; 24219-97-4; Mianserin-d3 hydrochloride; 1219804-97-3; 51152-88-6 ((S)-isomer)
Appearance
Solid powder
SMILES
CN1CCN2C(C1)C3=CC=CC=C3CC4=CC=CC=C42.Cl
InChi Key
YNPFMWCWRVTGKJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H20N2.ClH/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19;/h2-9,18H,10-13H2,1H3;1H
Chemical Name
5-methyl-2,5-diazatetracyclo[13.4.0.02,7.08,13]nonadeca-1(19),8,10,12,15,17-hexaene;hydrochloride
Synonyms
ORG GB-94 HCl; Mianserin; Depnon; Lerivon; Lumin; Lantanon; ORG GB-94 HCl; ORG GB 94 HCl; Norval; Tolvon
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~60 mg/mL (166.2~199.4 mM)
Water: ~30 mg/mL (~99.7 mM)
Ethanol: ~21 mg/mL (~69.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (8.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.3324 mL 1.6621 mL 3.3241 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05599126 Not yet recruiting Drug: Mianserin
Drug: Lorazepam
Depression Zhenghui YI December 2022 Phase 4
NCT02761161 Completed Drug: Mianserin
Behavioral: Imagery Rehearsal
Therapy
Post Traumatic Stress Disorder
Depression
Mental Health Services in the
Capital Region, Denmark
March 2016 Phase 4
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