Catalog Number: 4256
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
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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.
Background References
  1. 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
  2. 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
  3. Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception.
    Laughlin et al.
    J.Pharmacol.Exp.Ther., 2002;302:1168
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