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Thiocolchicoside GABA Receptor antagonist

Name: Thiocolchicoside
Brand: Selleck Chemicals
SKU: S5049
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5049

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.

Chemical Structure

Molecular Weight: 563.62

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Quality Control

Batch: Purity: 99.83%

99.83

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor TRP Channel Cholinesterase (ChE) GluR
Other GABA Receptor Inhibitors	Dihydromyricetin CGP52432 Pentylenetetrazol 4-Aminobutyric acid (GABA) (+)-Borneol Ginkgolide A Oxiracetam Emamectin Benzoate Fluralaner (-)-Borneol

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (177.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 33 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	563.62	Formula	C₂₇H₃₃NO₁₀S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	602-41-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	GABAA receptor
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. This compound 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. This chemical suppresses osteoclastogenesis induced by receptor activator of nuclear factor kappa-B ligand, breast cancer and multiple myeloma cells through inhibition of inflammatory pathways.
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. This compound 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.
References	[1] http://www.indjst.org/index.php/indjst/article/view/113409 [2] https://pubmed.ncbi.nlm.nih.gov/16806306/ [3] http://www.doublehelixresearch.com/files/journals/dhr-ijms/vol-4/issue-2/1.pdf

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-05-31)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06261320	ACTIVE_NOT_RECRUITING	Inflammatory Bowel Diseases	Polyclinique de l'Europe	2024-02-28	PHASE2
NCT05529290	COMPLETED	Temporomandibular Disorder	Yuzuncu Yil University	2019-07-16	PHASE4
NCT05261971	COMPLETED	Occlusion; Quality of Life	Yuzuncu Yil University	2018-12-01
NCT04110119	COMPLETED	Low Back Pain, Mechanical	Medipol University	2018-10-01	PHASE2
NCT00679146	COMPLETED	Low Back Pain	Sanofi	2008-04	PHASE3
NCT00917436	COMPLETED	Low Back Pain	Sanofi	2004-12	PHASE4

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