TPMPA

Catalog #: 1040
12 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
1040/10
1040/50

TPMPA | CAS No. 182485-36-5 | GABAA-rho Receptor Antagonists

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Description: Selective GABAA-ρ antagonist

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

Purity: ≥97%

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Product Details

Citations (12)

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Biological Activity

TPMPA is a selective, competitive GABA_A-ρ antagonist with only minimal effects on GABA_A and GABA_B receptors (K_b 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:

161.14

Formula:

C₆H₁₂NO₂P

Solubility:

Soluble to 100 mM in water

Purity:

≥97%

Storage:

Store at RT

CAS No:

182485-36-5

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

Differential signalling and glutamate receptor compositions in the OFF bipolar cell types in the mouse retina
T Ichinose, CB Hellmer
J. Physiol. (Lond.), 2016;594(4):883-94.
Glial glutamate transporter and glutamine synthetase regulate GABAergic synaptic strength in the spinal dorsal horn.
Jiang E, Yan X, Weng HR
J. Neurochem., 2012;121(4):526-36.
Activation of toll like receptor 4 attenuates GABA synthesis and postsynaptic GABA receptor activities in the spinal dorsal horn via releasing interleukin-1 beta.
Yan X, Jiang E, Weng H
J Neuroinflammation, 2015;12(0):222.
Neurogliaform cells dynamically regulate somatosensory integration via synapse-specific modulation.
Chittajallu, Ramesh, Pelkey, Kenneth, McBain, Chris J
Nat Neurosci, 2013;16(1):13-5.
GABA_C receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes.
Chebib et al.
Eur.J.Pharmacol., 1998;357:227
Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist.
Ragozzino et al.
Mol.Pharmacol., 1996;50:1024
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
The first selective antagonist for a GABA_c receptor.
Murata et al.
Bioorg.Med.Chem.Lett., 1996;6:2073

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for TPMPA

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

12 Citations: Showing 1 - 10

Neural Mechanisms Mediating Motion Sensitivity in Parasol Ganglion Cells of the Primate Retina.
Authors: Manookin Et al.
Neuron 2018;97:1327
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
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
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
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
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
Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction.
Authors: Antonelli Et al.
Nat Commun 2014;5:5066
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
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
Retinal input to efferent target amacrine cells in the avian retina.
Authors: Lindstrom Et al.
J Neurosci 2010;27:103

GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb.
Authors: Gascon Et al.
J Neurosci 2006;26:12956

The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Authors: Wood Et al.
Front Cell Neurosci 2000;131:1050

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