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Tandospirone (SM-3997) is a novel, highly potent and selective 5-HT1A receptor partial agonist with Ki of 27 nM, and exhibits selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Kis ranging from 1300-41000 nM). It has the potential to be used for treating the central nervous system disorders and the underlying mechanisms.
| Targets |
5-HT1A Receptor ( Ki = 27 nM )
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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]. |
| 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]. |
| 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 |
| References |
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| Molecular Formula |
C₂₁H₂₉N₅O₂
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|---|---|
| Molecular Weight |
383.49
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| Exact Mass |
383.23
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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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| Appearance |
Powder
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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 |
|---|---|
| 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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