Home Neuronal Signaling GABA Receptor antagonist Thiocolchicoside For research use only.

Thiocolchicoside

Synonyms: Thiocolchicine 2-glucoside analog, Coltramyl

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.

Thiocolchicoside Chemical Structure

Thiocolchicoside Chemical Structure

CAS No. 602-41-5

Purity & Quality Control

Thiocolchicoside Related Products

Signaling Pathway

GABA Receptor Signaling Pathways

GABA Receptor Signaling Pathway

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
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
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].
Animal Research Animal Models Male Sprague-Dawley CD rats
Dosages 10-30 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 563.62 Formula

C27H33NO10S
CAS No. 602-41-5 SDF --
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (177.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 33 mg/mL

Ethanol : Insoluble


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In vivo
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