Home Neuronal Signaling GABA Receptor antagonist Thiocolchicoside

research use only

Thiocolchicoside GABA Receptor antagonist

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.
Thiocolchicoside GABA Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 563.62

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 563.62 Formula

C27H33NO10S

 Storage (From the date of receipt)
CAS No. 602-41-5 -- Storage of Stock Solutions

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

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

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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
% DMSO
+
%

Calculation results:

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.

Mechanism of Action

Targets/IC50/Ki
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. 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[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. 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[1].
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map