| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes. It also functions as an H1 receptor inverse agonist/antihistamine. This multi-target profile underlies its antidepressant and sedative effects.
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| ln Vitro |
Setiptiline has demonstrated efficacy in preclinical behavioral models of depression. In animal studies, it showed antidepressant-like effects in forced swimming tests and tail suspension tests, consistent with its noradrenergic and serotonergic mechanisms of action. The compound's antihistaminic activity contributes to its sedative properties. Setiptiline has also been evaluated in combination with other psychotropic agents for the treatment of schizophrenia negative symptoms.
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| ln Vivo |
Setiptiline maleate shows dose-dependent antidepressant-like activity in rodent models. It has been evaluated in behavioral despair tests and has demonstrated efficacy in reducing immobility time, indicating antidepressant potential. Clinical studies in depressed patients have shown effectiveness in improving mood and anxiety symptoms, particularly in cases accompanied by insomnia. The compound's sedative effects are attributed to its H1 receptor antagonism.
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| Enzyme Assay |
The receptor binding affinity of Setiptiline maleate is typically assessed using radioligand binding assays with membrane preparations from transfected cells or native tissues expressing human or rodent α2-adrenergic, 5-HT2A, 5-HT2C, 5-HT3, and H1 receptors. Competitive binding experiments are performed using increasing concentrations of the test compound against specific radioligands (e.g., [³H]-rauwolscine for α2-adrenoceptors, [³H]-ketanserin for 5-HT2A). IC50 values are calculated and Ki values are derived using the Cheng-Prusoff equation.
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| Cell Assay |
Norepinephrine and serotonin reuptake inhibition is evaluated in cell-based assays using cell lines such as SK-N-SH neuroblastoma cells or HEK-293 cells expressing human serotonin or norepinephrine transporters. Cells are incubated with [³H]-norepinephrine or [³H]-serotonin in the presence of various concentrations of Setiptiline maleate. The amount of radiolabeled neurotransmitter taken up into cells is measured by scintillation counting, and IC50 values for reuptake inhibition are calculated. Antagonism of 5-HT2A and 5-HT3 receptors can be assessed using calcium flux assays in cells expressing these receptors.
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| Animal Protocol |
In vivo antidepressant activity is evaluated using rodent models such as the forced swimming test (FST) and tail suspension test (TST) in mice or rats. Setiptiline maleate is typically administered orally or intraperitoneally at various doses (e.g., 1-30 mg/kg) 30-60 minutes prior to testing. Immobility time is measured and compared to vehicle and positive control groups (e.g., imipramine or fluoxetine). Locomotor activity is assessed to exclude false positives from stimulant effects. The α2-adrenergic antagonist activity can be confirmed by reversal of clonidine-induced hypothermia or sedation in rodents.
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| ADME/Pharmacokinetics |
Setiptiline maleate is well absorbed after oral administration with good oral bioavailability. It is metabolized in the liver, primarily via cytochrome P450 enzymes, and has a plasma half-life suitable for once or twice daily dosing in humans. Plasma protein binding is moderate. The drug crosses the blood-brain barrier to exert its central effects. In depressed patients, age has been shown to affect plasma levels, with elderly patients potentially requiring dose adjustments. The maleate salt form is used to improve aqueous solubility and stability.
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| Toxicity/Toxicokinetics |
The most common adverse effects include sedation, drowsiness, dry mouth, and weight gain, consistent with its H1 antihistamine and serotonergic activities. Setiptiline is generally well-tolerated at therapeutic doses, though caution is advised when combining with other CNS depressants. Overdose may cause excessive sedation, confusion, and cardiovascular effects. Preclinical toxicology studies have shown a reasonable safety margin, with no significant organ toxicity at therapeutic exposures. The compound is contraindicated in patients with known hypersensitivity or those taking MAO inhibitors.
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| References |
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| Additional Infomation |
Setiptiline maleate is a maleate salt produced by reacting Setiptiline with an equivalent amount of maleic acid. It is an alpha-adrenergic antagonist and a serotonergic antagonist. It is a maleate salt and also a tetracyclic antidepressant. It contains Setiptiline (1+).
Setiptiline maleate (brand name: Tecipul®) was approved and marketed in Japan starting in 1989 for the treatment of depression. It is classified as a tetracyclic antidepressant (TeCA) and a noradrenergic and specific serotonergic antidepressant (NaSSA). The compound has also been investigated for the treatment of negative symptoms of schizophrenia. Its unique pharmacological profile—combining norepinephrine reuptake inhibition, α2-adrenergic antagonism, 5-HT2A/5-HT2C/5-HT3 antagonism, and H1 inverse agonism—distinguishes it from other antidepressants. The maleate salt (CAS# 85650-57-3) has a molecular weight of 377.43 and is soluble in DMSO. Storage is recommended at -20°C. |
| Molecular Formula |
C23H23NO4
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|---|---|
| Molecular Weight |
377.44
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| Exact Mass |
377.163
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| CAS # |
85650-57-3
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| Related CAS # |
Setiptiline;57262-94-9
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| PubChem CID |
5282470
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| Appearance |
White to gray solid powder
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| Boiling Point |
421.7ºC at 760 mmHg
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| Flash Point |
185.5ºC
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| LogP |
3.486
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
516
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCC2=C(C1)C3=CC=CC=C3CC4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
AVPIBVPBCWBXIU-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C19H19N.C4H4O4/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20;5-3(6)1-2-4(7)8/h2-9H,10-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;4-methyl-4-azatetracyclo[13.4.0.02,7.08,13]nonadeca-1(19),2(7),8,10,12,15,17-heptaene
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| Synonyms |
MO-8282; MO8282; MO 8282
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL (~264.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 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 (6.62 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6494 mL | 13.2471 mL | 26.4943 mL | |
| 5 mM | 0.5299 mL | 2.6494 mL | 5.2989 mL | |
| 10 mM | 0.2649 mL | 1.3247 mL | 2.6494 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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