Tofisopam |
Catalog No.GC40746
One-Click Copy Product Info
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2,3-벤조디아제핀 화합물인 토피소팜은 경구 활성 불안 완화제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 22345-47-7
Sample solution is provided at 25 µL, 10mM.
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Tofisopam is a 2,3-benzodiazepine anxiolytic agent. Tofisopam exerts its pharmacological effects by selectively inhibiting phosphodiesterase (PDE) isoenzymes (with IC50 values of 2.11μM for PDE-2A3, 1.98μM for PDE-3A, 0.42μM for PDE-4A1, and 0.92μM for PDE-10A1). Tofisopam can be used in research related to anxiety disorders, alcohol withdrawal syndrome, depression, as well as irritable bowel syndrome and bone metabolic diseases[1-4].
In vitro, L929 cells (mouse connective tissue cell line) were treated with Tofisopam (63μg/ml, 189μg/ml, 504μg/ml) for 2 hours. Tofisopam did not significantly increase the percentage of micronucleated binucleated cells, indicating no genotoxicity[5].
In vivo, female C57BL6J mice, starting at 10 weeks of age, received subcutaneous injections of Tofisopam (10mg/kg/day; 5 days per week) for 4 weeks. Tofisopam significantly increased trabecular thickness (Tb.Th) and bone volume fraction (BV/TV), and elevated the bone formation marker osteocalcin level[6]. In a psychosis model, Albino Swiss mice received intraperitoneal injections of Tofisopam (50mg/kg; twice daily; 5 days per week) for 19 days. Tofisopam significantly improved the prolonged immobility time in rats[7].
References:
[1] Bernard P, Dufresne-Favetta C, Favetta P, et al. Application of drug repositioning strategy to TOFISOPAM. Curr Med Chem. 2008;15(30):3196-203.
[2] Tóth M, Drabant S, Varga B, et al. Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam. Eur J Clin Pharmacol. 2008 Jan;64(1):93-4.
[3] Hovi-Viander M, Kanto J, Scheinin H, et al. Tofisopam and midazolam: differences in clinical effects and in changes of CSF monoamine metabolites. Br J Clin Pharmacol. 1985 Nov;20(5):492-6.
[4] Cameron MD, Wright J, Black CB, et al. In vitro prediction and in vivo verification of enantioselective human tofisopam metabolite profiles. Drug Metab Dispos. 2007 Oct;35(10):1894-902.
[5] Chłopkiewicz B, Ejchart A, Anuszewska E. Tofisopam--evaluation of mutagenic and genotoxic properties. Acta Pol Pharm. 2001 Jan-Feb;58(1):31-4.
[6] Bonnet N, Bernard P, Beaupied H, et al. Various effects of antidepressant drugs on bone microarchitectecture, mechanical properties and bone remodeling. Toxicol Appl Pharmacol. 2007 May 15;221(1):111-8.
[7] Rundfeldt C, Socała K, Wlaź P. The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25.
| Cell experiment [1]: | |
Cell lines | L929 cells (mouse connective tissue cell line) |
Preparation Method | L929 cells were grown in MEM (Eagle's minimum essential medium) supplemented with 10% foetal calf serum and antibiotics at 37°C in a humidified incubator containing 5% CO₂. L929 cells were treated with Tofisopam at concentrations of 63μg/ml, 189μg/ml, and 504μg/ml for 2 hours. |
Reaction Conditions | 63μg/ml, 189μg/ml, 504μg/ml; 2h |
Applications | Tofisopam at the used concentrations did not increase the percentage of micronucleated binucleated cells. |
| Animal experiment [2]: | |
Animal models | Female C57BL6J mice |
Preparation Method | Mice were acclimatized for two weeks and maintained under constant conditions. Starting at 12 weeks of age, mice received subcutaneous injections of Tofisopam (10mg/kg/day) 5 days per week for 4 weeks. At the end of the treatment, blood was collected after an overnight fast, and femurs were excised for analysis. |
Dosage form | 10mg/kg/day; subcutaneous injection; 5 days per week for 4 weeks |
Applications | Tofisopam significantly increased trabecular thickness (Tb.Th) and bone volume fraction (BV/TV), and elevated the bone formation marker osteocalcin level compared to the control group. |
References: | |
| Cas No. | 22345-47-7 | SDF | |
| Canonical SMILES | CCC1C(C=C2OC)=C(C(C3=CC(OC)=C(OC)C=C3)=NN=C1C)C=C2OC | ||
| Formula | C22H26N2O4 | M.Wt | 382.5 |
| Solubility | DMF: 2.5 mg/ml,DMSO: 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6144 mL | 13.0719 mL | 26.1438 mL |
| 5 mM | 522.9 μL | 2.6144 mL | 5.2288 mL |
| 10 mM | 261.4 μL | 1.3072 mL | 2.6144 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)