Catalog # Availability Size / Price Qty
TPMPA | CAS No. 182485-36-5 | GABAA-rho Receptor Antagonists
1 Image
Description: Selective GABAA-ρ antagonist

Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid

Purity: ≥97%

Product Details
Citations (12)
Supplemental Products

Biological Activity

TPMPA is 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

Soluble to 100 mM in water
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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. Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist.
    Ragozzino et al.
    Mol.Pharmacol., 1996;50:1024
  3. 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
  4. The first selective antagonist for a GABAc receptor.
    Murata et al.
    Bioorg.Med.Chem.Lett., 1996;6:2073

Product Datasheets

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Citations for TPMPA

The citations listed below are publications that use Tocris products. Selected citations for TPMPA include:

12 Citations: Showing 1 - 10

  1. Neural Mechanisms Mediating Motion Sensitivity in Parasol Ganglion Cells of the Primate Retina.
    Authors: Manookin Et al.
    Neuron  2018;97:1327
  2. A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina.
    Authors: Hellmer Et al.
    Physiol Rep  2018;6:e13885
  3. DA Regulation of GABAA Receptors Contributes to Light/Dark Modulation of the ON-Cone Bipolar Cell Receptive Field Surround in the Retina.
    Authors: Chaffiol Et al.
    Curr Biol  2017;27:2600
  4. Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
    Authors: Elgueta Et al.
    J Neurosci  2015;9:6
  5. The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina.
    Authors: Murphy-Baum and Taylor
    Vis Neurosci  2015;35:13336
  6. Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells.
    Authors: Vielma Et al.
    PLoS One  2014;9:e114330
  7. Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction.
    Authors: Antonelli Et al.
    Nat Commun  2014;5:5066
  8. Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa.
    Authors: Jensen
    PLoS One  2013;8:e79126
  9. Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome.
    Authors: Olmos-Serrano Et al.
    Br J Pharmacol  2010;30:9929
  10. Retinal input to efferent target amacrine cells in the avian retina.
    Authors: Lindstrom Et al.
    J Neurosci  2010;27:103


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