| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
5-HT1A Receptor ( Ki = 27 nM )
Tandospirone targets the 5-HT1A (serotonin) receptor with high affinity, exhibiting a Ki of 27 nM. It acts as a partial agonist, meaning it stimulates the receptor but with lower efficacy than a full agonist. This action on the 5-HT1A receptor is responsible for its anxiolytic and antidepressant effects. |
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| ln Vitro |
Tandospirone is roughly two to three orders of magnitude less potent than 5-HT1A at 5-HT2, 5-HT1C, α1-adrenergic, α2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM)[1].
Tandospirone is essentially inactive at beta-adrenergic, muscarinic cholinergic, 5-HT uptake sites, 5-HT1B receptors, and benzodiazepine receptors. Tandospirone inhibits protein kinase A (PKA)-mediated protein phosphorylation and neuronal activity by activating postsynaptic 5-HT1A receptor coupled with G-protein (Gi/o)[1]. In vitro, Tandospirone is characterized by its high affinity and selectivity for the 5-HT1A receptor. It has a Ki of 27 nM for 5-HT1A and is selective over other serotonin receptor subtypes. Its partial agonist activity is confirmed in functional assays, where it shows moderate efficacy in activating the receptor compared to a full agonist like serotonin. |
| ln Vivo |
Tandospirone (10-80 mg/kg; i.p.) inhibits freezing behavior in the rat model of conditioned fear stress-induced freezing behavior[3].
Tandospirone hows the anxiolytic effect dependent on the plasma concentration of at 0.5 hours but not 4 hours[3]. In vivo, Tandospirone has demonstrated anxiolytic and antidepressant activities in animal models. It has also been shown to significantly reduce haloperidol-induced bradykinesia (parkinsonian-like motor symptoms) in a dose-dependent manner, suggesting a potential role in treating extrapyramidal side effects. Its clinical efficacy is comparable to buspirone and about half that of diazepam. |
| Enzyme Assay |
The in vitro receptor binding assay for Tandospirone involves competitive binding studies. Membranes from cells expressing the 5-HT1A receptor are incubated with a radiolabeled ligand, such as [3H]-8-OH-DPAT, in the presence of varying concentrations of the compound. The amount of radioligand displaced is measured to determine the binding affinity (Ki).
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| Cell Assay |
In vitro cell-based functional assays for Tandospirone utilize cells expressing the 5-HT1A receptor, often a CHO or HEK293 cell line. The receptor is coupled to a G-protein, and its activation leads to the inhibition of adenylyl cyclase. Tandospirone's ability to inhibit forskolin-stimulated cAMP production is measured. The EC50, which indicates the potency of the partial agonist, is determined from the concentration-response curve.
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| Animal Protocol |
Seven-week-old male Sprague-Dawley rats (260-300 g), conditioned fear stress-induced freezing behavior rat model
10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg Intraperitoneal injection In vivo animal experiments for Tandospirone include standard models of anxiety, such as the elevated plus maze or the social interaction test in rats. The compound is administered orally or intraperitoneally, and its anxiolytic effect is measured by an increase in open-arm exploration or social behavior. Its antidepressant effects are assessed using the forced swim test or tail suspension test, where a reduction in immobility time indicates an antidepressant-like effect. |
| ADME/Pharmacokinetics |
Tandospirone has a molecular weight of 383.5 g/mol. It is typically administered orally and is well-absorbed. It is metabolized in the liver, and its metabolites are excreted in urine. Its half-life is relatively short, allowing for multiple daily dosing. It is stored as a powder at room temperature, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Toxicological data indicate that Tandospirone is generally well-tolerated. Common side effects include dizziness, drowsiness, and headache. Unlike benzodiazepines, it does not cause significant sedation, psychomotor impairment, or dependence, making it a safer alternative for long-term use. However, it can cause mild gastrointestinal disturbances.
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| References |
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| Additional Infomation |
Tandospirone is a dicarboxylidene imide compound with the chemical name (3aR,4S,7R,7aS)-hexahydro-1H-4,7-methyleneisoindole-1,3(2H)-dione, substituted at the 2-position with 4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl. It is a potent and selective partial agonist of the 5-HT1A receptor (Ki = 27 nM). It possesses antidepressant and anxiolytic pharmacological effects. Tandospirone belongs to the N-alkylpiperazine, N-arylpiperazine, pyrimidine, bridging, and dicarboxylidene imide classes. It is the conjugate base of tandospirone (1+). Tandospirone has been used in clinical trials for the treatment of schizophrenia.
Tandospirone is an approved drug in several countries, including Japan, where it is used for the treatment of anxiety and depression. It is not approved in the US or Europe. It is used in clinical research to study serotonergic mechanisms, anxiety, depression, and cognitive function. |
| Molecular Formula |
C₂₁H₂₉N₅O₂
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|---|---|
| Molecular Weight |
383.49
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| Exact Mass |
383.232
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| CAS # |
87760-53-0
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| Related CAS # |
Tandospirone citrate; 112457-95-1; Tandospirone hydrochloride; 99095-10-0
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| PubChem CID |
91273
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
613.9±65.0 °C at 760 mmHg
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| Melting Point |
112-113.5°
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| Flash Point |
325.1±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.589
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| LogP |
2.02
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
572
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1C[C@H]2C[C@@H]1[C@H]3[C@@H]2C(=O)N(C3=O)CCCCN4CCN(CC4)C5=NC=CC=N5
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| InChi Key |
CEIJFEGBUDEYSX-FZDBZEDMSA-N
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| InChi Code |
InChI=1S/C21H29N5O2/c27-19-17-15-4-5-16(14-15)18(17)20(28)26(19)9-2-1-8-24-10-12-25(13-11-24)21-22-6-3-7-23-21/h3,6-7,15-18H,1-2,4-5,8-14H2/t15-,16+,17+,18-
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| Chemical Name |
(1R,2S,6R,7S)-4-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dione
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| Synonyms |
SM-3997; SM3997; SM 3997; Tandospirone
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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: 16.7~26 mg/mL (43.5~67.8 mM)
Ethanol: ~15 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 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 (6.52 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 (6.52 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 | 2.6076 mL | 13.0381 mL | 26.0763 mL | |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01614041 | Completed | Drug: Usual dose treatment of Tandospirone Drug: Comparative high dose of tandospirone treatment |
Generalized Anxiety Disorder | Sumitomo Pharma (Suzhou) Co., Ltd. |
January 10, 2012 | Phase 4 |
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