Catalog Number: 1040
Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid
Biological Activity
A selective, competitive GABAA-ρ antagonist with only minimal effects on GABAA and GABAB receptors (Kb values are 2.1 μM (antagonist), 320 μM (antagonist) and EC50 ~ 500 μM (weak agonist) respectively). Displays 8-fold selectivity for human recombinant ρ1 receptors over ρ2 receptors.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water
  • Purity:
  • Storage:
    Store 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. GABAC receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes.
    Chebib et al.
    Eur.J.Pharmacol., 1998;357:227
  2. The involvement of GABA-C receptors in paired pulse depression of inhibitory postsynaptic currents in rat hippocampal CA1 pyramidal neurons.
    Xu et al.
    Exp.Neurol., 2009;216:243
  3. Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist.
    Ragozzino et al.
    Mol.Pharmacol., 1996;50:1024
  4. The first selective antagonist for a GABAc receptor.
    Murata et al.
    Bioorg.Med.Chem.Lett., 1996;6:2073
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