Cat. No. 4256
Chemical Name: (3R)-1-[4,4-Bis(3-methyl-2-thienyl)
Biological ActivityGABA 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.
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 / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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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