Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H29N5O2.C6H8O7 |
| Molecular Weight | 575.6108 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CC(O)(CC(O)=O)C(O)=O.O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN4CCN(CC4)C5=NC=CC=N5
InChI
InChIKey=DMLGUJHNIWGCKM-DPFKZJTMSA-N
InChI=1S/C21H29N5O2.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h3,6-7,15-18H,1-2,4-5,8-14H2;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t15-,16+,17+,18-;
| Molecular Formula | C21H29N5O2 |
| Molecular Weight | 383.4873 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | C6H8O7 |
| Molecular Weight | 192.1235 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/17516698|
https://www.ncbi.nlm.nih.gov/pubmed/11579010
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/17516698|
https://www.ncbi.nlm.nih.gov/pubmed/11579010
Sediel (generic name: tandospirone citrate, marketed as Sediel in Japan) is a new type of antianxiety drug developed independently by Sumitomo Pharmaceuticals. It acts selectively on only the serotonin nerves in the brain that play an important part in the formation of anxiety and depression, and demonstrates antianxiety and anti-depression effects. Since it does not act on the other nerves that are so extensive in the brain, there is virtually no hypnotic or sedative effect, and the drug displays virtually no drug-dependence or side effects such as drowsiness and dizziness. Sediel has been on sale in Japan since December 1996, and is recognized for recognized as effective in the treatment of generalized anxiety disorders. Tandospirone acts as a potent and selective 5-HT1A receptor partial agonist. It was also investigated the usefulness of 5-HT1A agonists for enhancing some types of cognitive performance and possibly social and work function in patients with schizophrenia, and related to this was discovered, that tandospirone in combination with atypical antipsychotic drugs can improve cognitive function in Schizophrenia.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1974152 |
27.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Sediel Approved UseUnknown Launch Date2003 |
|||
| Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9692774
Under voltage-clamp conditions, tandospirone (TDS) (3*10(-7) M) induced an inward rectifying K+ current in a concentration-dependent manner. In the inside-out patch recording mode, TDS-activated single K+ channel currents (iTDS) which also showed an inward rectification. When the GDP in cytosolic side was completely replaced with GTP, the open probability of iTDS significantly increased. These results indicate that the activation of 5-HT1A receptors by TDS directly opens the inward rectifying K+ channels via a G-protein mediated process.
| Substance Class |
Chemical
Created
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admin
on
Edited
Mon Mar 31 18:23:34 GMT 2025
by
admin
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Mon Mar 31 18:23:34 GMT 2025
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| Record UNII |
0R8E9BWM4J
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Validated (UNII)
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C28197
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C47794
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m10453
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CHEMBL274047
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SUB04674MIG
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BB-60
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145673
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32182
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112457-95-1
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DTXSID701350198
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C055267
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99095-12-2
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C74390
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60558
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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