Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C27H33NO10S |
Molecular Weight | 563.617 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OC)C2=C(CC[C@H](NC(C)=O)C3=CC(=O)C(SC)=CC=C23)C=C1O[C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O
InChI
InChIKey=LEQAKWQJCITZNK-AXHKHJLKSA-N
InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16-,19+,22+,23-,24+,27+/m0/s1
Molecular Formula | C27H33NO10S |
Molecular Weight | 563.617 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Thiocolchicoside is a muscle relaxant that has been authorised by national procedures in several EU Member States for use by mouth or injection into the muscles in the treatment of painful muscular disorders. Thiocolchicoside is marketed under the brand name Muscoril among others. Thiocolchicoside (TCC) is used clinically for its muscle relaxant, anti-inflammatory, and analgesic properties, and it has been shown to interact with gamma-aminobutyric acid (GABA) type A receptors (GABAARs) and strychnine-sensitive glycine receptors in the rat central nervous system.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16806306
Curator's Comment: Intraperitoneal injection of Thiocolchicoside in rats either alone or in combination with negative modulators of GABAergic transmission revealed convulsant and proconvulsant actions of this drug.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5347 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21054237 |
0.056 mM [IC50] | ||
1.9 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | Muscoril Approved UseMuscoril capsules and injections are used as an adjuvant treatment of painful muscle contractures in acute spinal pathology. |
PubMed
Title | Date | PubMed |
---|---|---|
Skin atrophy caused by thiocolchicoside injections. | 2006 Dec |
|
Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes. | 2007 Mar 8 |
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Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and gamma-aminobutyric acid receptors. | 2007 May 3 |
|
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://plaintips.com/muscoril
For oral use: The recommended and maximal dose of Muscoril (Thiocolchicoside) is 8 mg every 12 hours (i.e. 16 mg per day). The treatment duration is limited to 7 consecutive days.
For IM use: The recommended and maximal dose of Muscoril Injection is 4 mg every 12 hours (i.e. 8 mg per day). The treatment duration is limited to 5 consecutive days.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16806306
The phasic and tonic GABAAR-mediated currents recorded from Purkinje cells and granule neurons, respectively, in parasagittal cerebellar slices from adult male rats were inhibited by Thiocolchicoside in a concentration-dependent manner. The median inhibitory concentrations of Thiocolchicoside for these effects were approximately 0.15 and approximately 0.9 uM, respectively.
Substance Class |
Chemical
Created
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admin
on
Edited
Fri Dec 15 17:32:09 UTC 2023
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Fri Dec 15 17:32:09 UTC 2023
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Record UNII |
T1X8S697GT
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Record Status |
Validated (UNII)
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QM03BX05
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WHO-ATC |
M03BX05
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NCI_THESAURUS |
C29696
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WHO-ATC |
M03BX55
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C152589
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Thiocolchicoside
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C004280
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T1X8S697GT
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210-017-7
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m10747
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CHEMBL1705373
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