Product overview

Name Tiagabine hydrochloride
Purity >99%
Description Selective GAT-1 GABA uptake inhibitor
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Biological Data

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.

Solubility & Handling

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.

Calculators

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Chemical Data

Purity >99%
Chemical name (3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
Molecular Weight 412.01
Chemical structure Tiagabine hydrochloride  [145821-59-6] Chemical Structure
Molecular Formula C20H25NO2S2.HCl
CAS Number 145821-59-6
PubChem identifier 91274
SMILES CC1=C(SC=C1)C(=CCCN2CCC[C@H](C2)C(=O)O)C3=C(C=CS3)C.Cl
InChi InChI=1S/C20H25NO2S2.ClH/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23;/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23);1H/t16-;/m1./s1
InChiKey YUKARLAABCGMCN-PKLMIRHRSA-N
MDL number MFCD07369025

References for Tiagabine hydrochloride

References are publications that support the biological activity of the product
  • 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.
  • 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.
  • 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.

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