Overview

  • Product name

    Tiagabine hydrochloride, GAT-1 inhibitor
  • Description

    Selective GAT-1 inhibitor
  • Alternative names

    • Gabitril
    • NNC 05-328
  • Biological description

    GABA uptake inhibitor, selective for GAT-1. Anticonvulsant in vivo.

    Also available in simple stock solutions (ab146701) - add 1 ml of water to get an exact, ready-to-use concentration.
  • Purity

    > 99%
  • CAS Number

    115103-54-3
  • Chemical structure

    Chemical Structure

Properties

Images

  • Tiagabine restored LTD via the activation of GABAB receptors in LPS animals.

    Tiagabine (20 µM) and/or CGP55845 (1 µM) were applied in the perfusate during both the recording of baseline activity and LFS (1 Hz stimulation, 15 min) delivery. (Panel A) Time-course and recapitulative graph depicting LTD induction in control (SAL) animals. LFS induced an LTD of fEPSP amplitude in control animals (SAL; filled circles; N = 8), which was significantly blocked by the GABAB receptor antagonist CGP55845 (SAL+CGP; open circles; N = 5; * p<0.05 vs SAL group). Tiagabine had no significant effect on LTD level (SAL+T; filled triangles; N = 8).

References

This product has been referenced in:

  • Borden LA  et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol 269:219-24 (1994). Read more (PubMed: 7851497) »
  • Suzdak PD  et al. Quantitative autoradiographic characterization of the binding of [3H]tiagabine (NNC 05-328) to the GABA uptake carrier. Brain Res 647:231-41 (1994). Read more (PubMed: 7922499) »
  • Andersen KE  et al. 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-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate. J Med Chem 36:1716-25 (1993). Read more (PubMed: 8510100) »
See all 2 Publications for this product

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