| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
- `Setiptiline` is a norepinephrine (NE) reuptake inhibitor with binding affinity for 5-hydroxytryptamine 2 (5-HT₂) receptors and histamine H₁ receptors. Its Ki values are: 25 nM for NE transporter (NET), 18 nM for 5-HT₂ receptors, and 8 nM for H₁ receptors [4]
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|---|---|
| ln Vitro |
- In rat brain synaptosome preparations, `Setiptiline` (0.1-100 nM) concentration-dependently inhibited [³H]-NE reuptake, with an IC₅₀ of 32 nM; 100 nM `Setiptiline` inhibited reuptake by 85 ± 4% compared to the control group [4]
- In human recombinant 5-HT₂ receptors, `Setiptiline` (1-100 nM) displaced [³H]-ketanserin with a Ki of 18 nM; in rat brain H₁ receptor preparations, it displaced [³H]-pyrilamine with a Ki of 8 nM [4] - `Setiptiline` (up to 1 μM) did not significantly inhibit [³H]-5-HT reuptake in rat brain synaptosomes [4] |
| ln Vivo |
- In mice forced swim test (FST), oral `Setiptiline` (10, 20, 40 mg/kg) reduced immobility time by 25 ± 3%, 40 ± 5%, and 55 ± 4%, respectively, compared to the vehicle group; the effect was comparable to imipramine (20 mg/kg, 45 ± 4% reduction) [1]
- In rats with learned helplessness (LH) model, intraperitoneal `Setiptiline` (5, 10 mg/kg/day) for 7 days reversed escape deficit: escape latency decreased from 180 ± 15 s (model group) to 90 ± 10 s (10 mg/kg group), and escape success rate increased from 20 ± 3% to 75 ± 5% [4] - In 30 depressed patients with schizophrenia (on antipsychotics), oral `Setiptiline` (12.5-50 mg/day) for 8 weeks improved negative symptoms: Scale for the Assessment of Negative Symptoms (SANS) total score decreased from 65 ± 8 to 42 ± 6, with reduced blunted affect and avolition (p < 0.05) [3] |
| Enzyme Assay |
- NE reuptake inhibition assay: Rat brain cortex synaptosomes were suspended in Krebs-Ringer buffer (pH 7.4). The 0.5 mL assay mixture contained synaptosomes (50 μg protein), [³H]-NE (5 nM), and `Setiptiline` (0.1-100 nM). After 10 min incubation at 37℃, the reaction was terminated by filtration. Filters were washed, radioactivity was counted, and IC₅₀ was calculated [4]
- 5-HT₂ receptor binding assay: Human recombinant 5-HT₂ receptor membranes (HEK293 cells) were used. The 0.2 mL mixture contained membrane protein (10 μg), [³H]-ketanserin (0.5 nM), and `Setiptiline` (1-100 nM). After 60 min incubation at 25℃, filtration and counting were performed, and Ki was calculated via Cheng-Prusoff equation [4] |
| Animal Protocol |
- Mouse FST: Male ICR mice (20-25 g) received oral `Setiptiline` (10, 20, 40 mg/kg). 60 min later, mice were placed in a 25℃ water tank (20 cm diameter, 15 cm depth) for 6 min; immobility time was recorded in the last 4 min [1]
- Rat LH model: Male Sprague-Dawley rats (250-300 g) received inescapable foot shocks for 2 days to induce LH. Then, intraperitoneal `Setiptiline` (5, 10 mg/kg) was given daily for 7 days. On day 8, escape latency and success rate were measured in a shuttle box [4] |
| ADME/Pharmacokinetics |
In patients with depression, oral thiotetriptyline maleate (15-30 mg/day) showed age-related plasma concentrations: steady-state plasma concentrations were 25 ± 5 ng/mL in young patients (20-40 years) and 48 ± 7 ng/mL in older patients (65-80 years); apparent oral clearance (CL/F) was 3.2 ± 0.5 L/h (young group) and 1.7 ± 0.3 L/h (older group), respectively, with no significant difference in t₁/₂ (18 ± 2 h vs. 20 ± 3 h) [2] In rats, oral bioavailability of thiotetriptyline (20 mg/kg) was 65 ± 5%, Cmax was 1.2 ± 0.1 μg/mL (2 hours after administration), t₁/₂ was 12 ± 1 h, and brain/plasma ratio was 3.5 ± 0.3 [4]
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| Toxicity/Toxicokinetics |
The plasma protein binding rate of sertriptyline in human plasma is 92 ± 2% (ultrafiltration method), and it is not significantly replaced by commonly used antidepressants or antipsychotics [4]
- 45 patients with depression were treated with sertriptyline (15-30 mg/day) for 4 weeks. Common side effects included drowsiness (35%), dry mouth (20%), and constipation (15%). No significant changes in liver and kidney function (ALT, AST, BUN, creatinine) were observed [2] - In mice, the oral LD₅₀ of sertriptyline was 350 ± 25 mg/kg, and the intraperitoneal LD₅₀ was 120 ± 10 mg/kg. High doses can cause sedation, ataxia, and respiratory depression [4] |
| References |
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| Additional Infomation |
Setiptiline is a tetracyclic antidepressant with the chemical name 2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine, containing a methyl group at the 2-position. Its maleate is used in Japan to treat depression. It has both alpha-adrenergic and serotonergic antagonist effects. It is a tetracyclic antidepressant and also a tertiary amine compound. It is the conjugate base of Setiptiline (1+). Setiptiline is a tetracyclic antidepressant (TeCA) that is both a norepinephrine and a specific serotonergic antidepressant (NaSSA). In Japan, Mochida Pharmaceuticals began commercializing the drug for the treatment of depression in 1989.
Drug Indications For the treatment of depression. Used for the treatment of depression. Mechanism of Action Sertriptyline is an antagonist of both α2-adrenergic and serotonin receptors. Antagonism of α2 receptors may relieve presynaptic inhibition of adrenergic neurotransmission, allowing for a more complete and sustained release of norepinephrine into the synaptic cleft. Antagonism of serotonin receptors may lead to receptor upregulation, ultimately enhancing serotonergic signaling. The exact physiological mechanism behind sertriptyline's antidepressant effect is unclear, but the above possibilities are plausible explanations. Pharmacodynamics Sertriptyline is a tetracyclic antidepressant. It is used to relieve symptoms of major depressive disorder. - `Certiline` is a tetracyclic antidepressant (TeCA) used to treat major depressive disorder. Its mechanism of action is through inhibiting norepinephrine (NE) reuptake and blocking 5-HT₂/H₁ receptors [1][4] - `Certiline` can be used in combination with antipsychotic drugs to treat negative symptoms of schizophrenia, improve emotional blunting/diminished will, and does not aggravate positive symptoms [3] - `Certiline` is the first-line drug for treating patients with depression accompanied by insomnia due to its H₁ receptor-mediated sedative effect [2][4] |
| Molecular Formula |
C19H19N
|
|---|---|
| Molecular Weight |
261.36086
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| Exact Mass |
261.152
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| CAS # |
57262-94-9
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| Related CAS # |
Setiptiline maleate;85650-57-3;Setiptiline-d3;1795024-97-3
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| PubChem CID |
5205
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| Appearance |
White to off-white solid powder
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| Density |
1.15
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| Boiling Point |
421.7ºC at 760mmHg
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| Flash Point |
185.5ºC
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| Index of Refraction |
1.656
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| LogP |
3.775
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
397
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GVPIXRLYKVFFMK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19N/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20/h2-9H,10-13H2,1H3
|
| Chemical Name |
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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| 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) |
DMSO : ~25 mg/mL (~95.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.57 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 | 3.8261 mL | 19.1307 mL | 38.2614 mL | |
| 5 mM | 0.7652 mL | 3.8261 mL | 7.6523 mL | |
| 10 mM | 0.3826 mL | 1.9131 mL | 3.8261 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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