Tiagabine hydrochloride

Name: Tiagabine hydrochloride
Brand: Tocris Bioscience
SKU: 4256

Tocris Bioscience, part of Bio-Techne | Catalog # 4256

Citations (5)

COA / SDS

Selective GAT-1 inhibitor; anticonvulsant

Key Product Details

Description:	Selective GAT-1 inhibitor; anticonvulsant
Chemical Name:	(3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	412.01

View Full Technical Details for Tiagabine hydrochloride

Technical Data
Citations

Biological Activity for Tiagabine hydrochloride

Tiagabine hydrochloride is a GABA uptake inhibitor (IC₅₀ = 67 nM in vivo). Exhibits high affinity and selectivity for the GAT-1 GABA transporter. Anticonvulsant; also attenuates established dynorphin-induced allodynia in a mouse model after systemic administration.

Compound Libraries for Tiagabine hydrochloride

Tiagabine hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Tiagabine hydrochloride

M. Wt	412.01
Formula	C₂₀H₂₅NO₂S₂.HCl
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	145821-59-6
PubChem ID	91274
InChi Key	YUKARLAABCGMCN-PKLMIRHRSA-N
Smiles	CC3=C(SC=C3)/C(C2=C(C)C=CS2)=C\CCN1C[C@H](C(O)=O)CCC1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Tiagabine hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	20.6	50
	DMSO	41.2	100

Preparing Stock Solutions for Tiagabine hydrochloride

The following data is based on the product molecular weight 412.01.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.43 mL	12.14 mL	24.27 mL
5 mM	0.49 mL	2.43 mL	4.85 mL
10 mM	0.24 mL	1.21 mL	2.43 mL
50 mM	0.05 mL	0.24 mL	0.49 mL

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References for Tiagabine hydrochloride

References are publications that support the biological activity of the product.

Dhar Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA updake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J.Med.Chem. 1994 PMID: 8057281
Laughlin Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabap. in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 2002 PMID: 12183677
Andersen The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug ca J.Med.Chem. 1993 PMID: 8510100