Catalog Number: 1081
Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Biological Activity
A potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • 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.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. Orally active and potent inhibitors of γ-aminobutyric acid.
    Ali et al.
    J.Med.Chem., 1985;28:653
  2. Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1.
    Krause and Schwarz
    Mol.Pharmacol., 2005;68:1728
  3. On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A.
    Murali Dha
    Bioorg.Med.Chem.Lett., 1996;6:1535
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