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Tiagabine hydrochloride


Product overview

  • Name
    Tiagabine hydrochloride
  • Short description
    Selective GAT-1 GABA uptake inhibitor
  • Biological description
    Selective GAT-1 GABA uptake inhibitor (IC50 = 67 nM). Selective for GAT-1 over mGAT2, mGAT3 and mGAT4 (IC50 values are 0.8, 300, >300 and 800 µM respectively). Shows anticonvulsive, antinociceptive, anxiolytic and antidepressant actions. Blood-brain barrier permeable.
  • Biological action
  • Purity
  • Citations


  • Chemical name
    (3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
  • Molecular Weight
  • Chemical structure
    Tiagabine hydrochloride  [145821-59-6]
  • Molecular Formula
  • CAS Number
  • PubChem identifier
  • InChi
  • InChiKey
  • MDL number

Storing and Using Your Product

  • Storage instructions
    Room temperature (desiccate)
  • Solubility overview
    Soluble in water (50mM) and in DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for Tiagabine hydrochloride

  • Long-term anxiolytic and antidepressant-like behavioural effects of tiagabine, a selective GABA transporter-1 (GAT-1) inhibitor, coincide with a decrease in HPA system activity in C57BL/6 mice.

    Thoeringer CK et al (2010) J Psychopharmacol 24(5) : 733-43.
    PubMedID: 19346277
  • Correlation between anticonvulsant activity and inhibitory action on glial gamma-aminobutyric acid uptake of the highly selective mouse gamma-aminobutyric acid transporter 1 inhibitor 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and its N-alkyla

    White HS et al (2002) J Pharmacol Exp Ther 302(2) : 636-44.
    PubMedID: 12130726
  • Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception.

    Laughlin TM et al (2002) J Pharmacol Exp Ther 302(3) : 1168-75.
    PubMedID: 12183677
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