Tandospirone citrate
Based on 3 publication(s) in Google Scholar
Tandospirone (SM-3997) citrate is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone citrate has anxiolytic and antidepressant activities. Tandospirone citrate can be used for the research of the central nervous system disorders and the underlying mechanisms.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 112457-95-1
- Formula: C27H37N5O9
- Molecular Weight:575.61
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tandospirone citrate
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT1A Receptor |
Tandospirone citrate 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 citrate is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors[1].
Tandospirone citrate 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 citrate 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 112457-95-1
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Appearance Solid
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Molecular Weight 575.61
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Formula C27H37N5O9
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Color White to off-white
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SMILES
O=C1N(CCCCN2CCN(C3=NC=CC=N3)CC2)C([C@@]4([H])[C@](C5)([H])CC[C@]5([H])[C@@]14[H])=O.O=C(CC(C(O)=O)(O)CC(O)=O)O
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Synonyms
SM-3997 citrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvent & Solubility
H2O : 29.17 mg/mL (50.68 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 25 mg/mL (43.43 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O | 1 mM | 1.7373 mL | 8.6864 mL | 17.3729 mL | 43.4322 mL |
| 5 mM | 0.3475 mL | 1.7373 mL | 3.4746 mL | 8.6864 mL | |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7373 mL | 4.3432 mL | |
| 15 mM | 0.1158 mL | 0.5791 mL | 1.1582 mL | 2.8955 mL | |
| 20 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1716 mL | |
| 25 mM | 0.0695 mL | 0.3475 mL | 0.6949 mL | 1.7373 mL | |
| 30 mM | 0.0579 mL | 0.2895 mL | 0.5791 mL | 1.4477 mL | |
| 40 mM | 0.0434 mL | 0.2172 mL | 0.4343 mL | 1.0858 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3475 mL | 0.8686 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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