| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
α2-adrenergic receptor ( pKi = 6.95 ); 5-HT3 Receptor ( pKi = 8.1 ); 5-HT2 Receptor ( pKi = 8.05 ); H1 Receptor ( pKi = 9.3 )
(R)-Mirtazapine targets the 5-HT3 receptor as a selective antagonist. It is mainly metabolized by CYP3A4. Unlike the parent compound, which is a 5-HT2/3 receptor inhibitor, (R)-Mirtazapine demonstrates potential in modulating pain perception through serotonergic pathways. It is a potential analgesic agent. |
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| ln Vitro |
In vitro, (R)-Mirtazapine is a 5-HT3 receptor antagonist. It is the R(-)-enantiomer of Mirtazapine. Its activity makes it a valuable tool for studying the role of 5-HT3 receptors in pain perception and other physiological processes. Its antinociceptive properties have been demonstrated in animal models.
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| ln Vivo |
The unique noradrenergic and specific serotonergic antidepressant mirtazapine acts antinociceptive. It is optically active and currently marketed as racemate. In an animal model of acute pain it has been shown that the enantiomers exhibit differential effects: the R(-)-enantiomer showed anti-, the S(+)-enantiomer pronociceptive properties while the racemate acted antinociceptive at low doses and profoundly pronociceptive after high-dose application. Aim of the present study was to evaluate potential enantioselective effects of mirtazapine in neuropathic pain. In a chronic constriction injury model of neuropathic pain, Wistar rats were injected (+/-)-mirtazapine and the enantiomers intrathecally. All substances were dosed between 0.001 and 1mg/kg and compared to vehicle in a randomized and blinded approach. Thermal hyperalgesia and mechanical allodynia were assessed. In contrast to the acute pain results, only racemic mirtazapine exerted significant sustained analgesic effects up to 48 h. Antinociception was observed at all dosages with a maximum in the range of 0.01 mg/kg. Surprisingly, neither enantiomer was pro- nor antinociceptive at any dose or time. Our findings suggest that the synergism of both enantiomers is required to evoke a significant analgesic effect for the treatment of neuropathic pain. Our study gained no evidence for the use of either R(-) nor S(+)-mirtazapine alone. Due to the unique characteristics of (+/-)-mirtazapine and its proven efficacy in acute pain our results suggest that racemic mirtazapine may be a particularly useful antidepressant in the adjunctive treatment of chronic neuropathic pain states and could provide additional benefit to current therapeutic options[1].
In vivo, (R)-Mirtazapine has antinociceptive properties in animal models of acute thermal nociception. It is mainly metabolized by CYP3A4. Its primary application is in the treatment of major depressive disorder. Its unique pharmacological profile allows it to be effective not only as an antidepressant but also for anxiety disorders. |
| Enzyme Assay |
In vitro receptor binding assays for (R)-Mirtazapine involve measuring its affinity for 5-HT3 receptors. Radioligand binding studies using ³H-BRL43694 or other 5-HT3 ligands are performed on membranes from cells expressing the receptor. The compound is incubated with increasing concentrations, and Ki values are calculated. Functional assays measure its ability to antagonize 5-HT3 receptor-mediated ion flux.
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| Cell Assay |
For in vitro cell-based assays, cells expressing 5-HT3 receptors are cultured and treated with (R)-Mirtazapine at various concentrations. Receptor antagonism is confirmed by its ability to block serotonin-induced calcium influx or ion flux. Cell viability is assessed by standard assays. The compound's effects on pain-related signaling pathways can be assessed in neuronal cell cultures.
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| Animal Protocol |
In vivo animal studies with (R)-Mirtazapine are conducted in models of pain and depression. The compound is administered orally or intraperitoneally. Antinociceptive effects are assessed using behavioral tests such as the hot plate test or tail flick test. Antidepressant-like effects are assessed using the forced swim test or tail suspension test.
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| ADME/Pharmacokinetics |
(R)-Mirtazapine (CAS: 61364-37-2) has a molecular weight of 265.35 g/mol and a molecular formula of C17H19N3. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C. The compound is the R-enantiomer of Mirtazapine and a 5-HT3 receptor antagonist.
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| Toxicity/Toxicokinetics |
(R)-Mirtazapine is a research compound and is not approved for human therapeutic use as a single enantiomer. In preclinical studies, it has shown a manageable safety profile. As a 5-HT3 receptor antagonist, it may have effects on gastrointestinal function and pain perception. Standard laboratory safety precautions should be followed when handling the compound.
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| Additional Infomation |
LSM-5894 is an organic heterobicyclic compound and an organic nitrogen heterocyclic compound.
See also: Mirtazapine (note moved to). (R)-Mirtazapine ((R)-Org3770) is the R(-)-enantiomer of Mirtazapine, a 5-HT3 receptor antagonist with antinociceptive properties. It has the CAS number 61364-37-2 and a molecular weight of 265.35 g/mol. It is not FDA-approved as a single enantiomer and is intended for research use only. |
| Molecular Formula |
C₁₇H₁₆D₃N₃
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|---|---|
| Molecular Weight |
265.35
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| Exact Mass |
265.157
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| CAS # |
61364-37-2
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| Related CAS # |
Mirtazapine;85650-52-8;(S)-Mirtazapine;61337-87-9;(S)-Mirtazapine-d3;Mirtazapine-d3;1216678-68-0;(R)-Mirtazapine-d3
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| PubChem CID |
3085219
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
432.4±45.0 °C at 760 mmHg
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| Flash Point |
215.3±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.668
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| LogP |
2.75
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
345
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N12C3C(=CC=CN=3)CC3C=CC=CC=3[C@@H]1CN(C)CC2
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| InChi Key |
RONZAEMNMFQXRA-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C17H19N3/c1-19-9-10-20-16(12-19)15-7-3-2-5-13(15)11-14-6-4-8-18-17(14)20/h2-8,16H,9-12H2,1H3/t16-/m0/s1
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| Chemical Name |
(7R)-5-methyl-2,5,19-triazatetracyclo[13.4.0.02,7.08,13]nonadeca-1(15),8,10,12,16,18-hexaene
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| Synonyms |
(R)-Mirtazapine; 61364-37-2; R-Mirtazapine; (-)-Mirtazapine; R-(-)-Mirtazapine; Org 44-19; 0UF1VD57JD; (R)-1,2,3,4,10,14b-Hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine;
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7686 mL | 18.8430 mL | 37.6861 mL | |
| 5 mM | 0.7537 mL | 3.7686 mL | 7.5372 mL | |
| 10 mM | 0.3769 mL | 1.8843 mL | 3.7686 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.
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.
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