Home Neuronal Signaling GABA Receptor inhibitor Tiagabine For research use only.

Tiagabine

Synonyms: Gabitril, NO050328, NO328, TGB

Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

Tiagabine Chemical Structure

Tiagabine Chemical Structure

CAS No. 115103-54-3

Purity & Quality Control

Tiagabine Related Products

Signaling Pathway

GABA Receptor Signaling Pathways

GABA Receptor Signaling Pathway

Biological Activity

Description Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Targets
GABA reuptake [1]
In vitro
In vitro Tiagabine is a potent inhibitor of GABA uptake into neurons and glial cells. It is involved in modulating GABA levels, especially in areas such as the hippocampus and thalamus[2]. Tiagabine not only affected the decay kinetics of the IPSCs, it also reduced the frequency of occurrence of both spontaneous and miniature IPSCs[1].
In Vivo
In vivo Tiagabine offers a significant neuroprotection in global ischemia in gerbils when given 30 min before ischemia but not when given 3 h after ischemia[3].
Animal Research Animal Models Male adult Sprague-Dawley rats
Dosages 0.2 μmol
Administration microinjected unilaterally into the globus pallidus
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04455841 Recruiting
Anemia|Post-essential Thrombocythemia Myelofibrosis|Post-polycythemia Vera Myelofibrosis
Incyte Corporation
 March 19 2021 Phase 1|Phase 2
NCT04021355 Recruiting
Obesity|Hypertension|Circadian Dysregulation|Salt; Excess
University of Alabama at Birmingham
 July 14 2020 Not Applicable
NCT01904487 Completed
Alcoholism
Rajesh Narendran|University of Pittsburgh
 April 19 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 375.55 Formula

C20H25NO2S2
CAS No. 115103-54-3 SDF Download Tiagabine SDF
Density 1.208 g/mL
Smiles CC1=C(SC=C1)C(=CCCN2CCCC(C2)C(=O)O)C3=C(C=CS3)C
Storage (From the date of receipt) 2 years 4°C liquid

In vitro
Batch:

DMSO : 75 mg/mL ( (199.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 75 mg/mL

Ethanol : 75 mg/mL


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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