Tiagabine hydrochloride

Cat. No. 4256

Tiagabine hydrochloride C20H25NO2S2.HCl [145821-59-6]

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Chemical Name: (3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride

Biological Activity

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.

Technical Data

Soluble to 50 mM in water and to 100 mM in DMSO
>99 %
Desiccate at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Laughlin et al (2002) Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 302 1168. PMID: 12183677.

Dhar et al (1994) 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. 37 2334. PMID: 8057281.

Andersen et al (1993) 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 candidate. J.Med.Chem. 36 1716. PMID: 8510100.

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Keywords: Tiagabine hydrochloride, supplier, antiepileptic, anticonvulsants, gaba, transporters, uptake, inhibitors, inhibits, gat-1, selective, antinociception, antinociceptive, Tocris Bioscience, GABA Inhibitor products

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