Thiocolchicoside

For research use only.

Catalog No.S5049 Synonyms: Thiocolchicine 2-glucoside analog, Coltramyl

Thiocolchicoside Chemical Structure

CAS No. 602-41-5

Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.

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Biological Activity

Description Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
Targets
GABAA receptor [2]
()
In vitro

Thiocolchicoside exhibits a selective affinity for the inhibitory gamma-aminobutyric acid and glycinergic receptors. It has an agonistic action at the spinal-strychnine-sensitive receptors that could mediate its myorelaxant effect. It might preferentially interact with a cortical subtype of the gamma-aminobutyric acid type A (GABAA) receptor that expresses low-affinity binding sites for GABA. GABAB receptors are largely unaffected by thiocolchicoside and hence do not contribute to its muscle relaxation action. Thiocolchicoside suppresses osteoclastogenesis induced by receptor activator of nuclear factor kappa-B ligand, breast cancer and multiple myeloma cells through inhibition of inflammatory pathways[3].

In vivo Thiocolchicoside is used as muscle relaxant agent without any side effects. It is rapidly absorbed from the gastrointestinal tract, undergoes first pass metabolism with an oral bioavailability of about 25 % and a biological half-life of 5-6 h. Thiocolchicoside is broken down in the body to a metabolite called 3-demethylthiocolchicine that could damage cells therefore inducing toxicity in the embryo, neoplastic changes and fertility reduction in male. Local skin preparations are less toxic[1].

Protocol

Animal Research:

[2]

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  • Animal Models: Male Sprague-Dawley CD rats
  • Dosages: 10-30 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (177.42 mM)
Water 100 mg/mL (177.42 mM)
Ethanol 2 mg/mL (3.54 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 563.62
Formula

C27H33NO10S

CAS No. 602-41-5
Storage powder
in solvent
Synonyms Thiocolchicine 2-glucoside analog, Coltramyl
Smiles CC(=O)NC1CCC2=CC(=C(C(=C2C3=CC=C(C(=O)C=C13)SC)OC)OC)OC4C(C(C(C(O4)CO)O)O)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID