Tandospirone
Based on 3 publication(s) in Google Scholar
Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.41%
- CAS. Nr.: 87760-53-0
- Formel: C21H29N5O2
- Molecular Weight:383.49
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Tandospirone
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Biologische Aktivität
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5-HT1A Receptor 27 nM (Ki) |
5-HT1A Receptor |
Tandospirone is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, α1-adrenergic, α2-adrenergic and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM) than 5-HT1A[1].
Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors[1].
Tandospirone activates postsynaptic 5-HT1A receptor coupled with G-protein (Gi/o), resulting in inhibition of protein kinase A (PKA)-mediated protein phosphorylation and neuronal activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tandospirone exhibits the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Seven-week-old male Sprague-Dawley rats (260-300 g), conditioned fear stress-induced freezing behavior rat model[3]
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Dosage:10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg
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Administration:Intraperitoneal injection
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Result:Inhibited freezing behavior in a dose-dependent manner.
Chemical Information
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CAS. Nr. 87760-53-0
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Appearance Solid
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Molecular Weight 383.49
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Formel C21H29N5O2
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Color White to off-white
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SMILES
O=C1[C@]2([H])[C@]([C@H]3CC[C@@H]2C3)([H])C(N1CCCCN(CC4)CCN4C5=NC=CC=N5)=O
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Synonyms
SM-3997
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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NPJ Digit Med
Tandospirone augments cisplatin treatment by lowering cholesterol and managing distress in NSCLC patients. [Abstract]2025 Nov 17;8(1):663. PMID: 41249389 -
Pharmacology
Pharmacological Characteristics of Anxiolytics on Acetylcholine-Induced Contractions in Rat Detrusor Smooth Muscle. [Abstract]2020;105(7-8):369-376. PMID: 31655826 -
Neurosci Lett
Pre-treatment with Tandospirone attenuates fentanyl-induced respiratory depression without affecting the analgesic effects of fentanyl in rodents. [Abstract]2022 Feb 6:771:136459. PMID: 35041907
Lösungsmittel & Löslichkeit
DMSO : 16.67 mg/mL (43.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hamik A, et al. Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites. Biol Psychiatry. 1990 Jul 15;28(2):99-109. [Content Brief]
[2]. Xuefei Huang, et al. Role of tandospirone, a 5-HT1A receptor partial agonist, in the treatment of central nervous system disorders and the underlying mechanisms. Oncotarget. 2017 Nov 24; 8(60): 102705–102720. [Content Brief]
[3]. Kyoko Nishitsuji, et al. The pharmacokinetics and pharmacodynamics of tandospirone in rats exposed to conditioned fear stress. Eur Neuropsychopharmacol. 2006 Jul;16(5):376-82. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | 65.1907 mL |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | 13.0381 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL | 6.5191 mL | |
| 15 mM | 0.1738 mL | 0.8692 mL | 1.7384 mL | 4.3460 mL | |
| 20 mM | 0.1304 mL | 0.6519 mL | 1.3038 mL | 3.2595 mL | |
| 25 mM | 0.1043 mL | 0.5215 mL | 1.0431 mL | 2.6076 mL | |
| 30 mM | 0.0869 mL | 0.4346 mL | 0.8692 mL | 2.1730 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6519 mL | 1.6298 mL |
Tandospirone Related Classifications
HY-14558 Related Classifications
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