Tiagabine hydrochloride
Chemical Name: (3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
Purity: ≥99%
Biological Activity
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.Technical Data
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.
Background References
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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.
Dhar et al.
J.Med.Chem., 1994;37:2334 -
Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabap. in mouse models of acute, prolonged, and chronic nociception.
Laughlin et al.
J.Pharmacol.Exp.Ther., 2002;302:1168 -
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
Andersen et al.
J.Med.Chem., 1993;36:1716
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Citations for Tiagabine hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Tiagabine hydrochloride include:
2 Citations: Showing 1 - 2
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Neonatal brain injury causes cerebellar learning deficits and Purkinje cell dysfunction.
Authors: Sathyanesan
Nature Communications 2018;9(1):3235
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GAT-1 mediated GABA uptake in rat oligodendrocytes.
Authors: María Victoria Et al.
Glia 2017;65:514-522
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