TPMPA

Catalog # 1040

Citations (12)

(1)

COA / SDS

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Key Product Details

Description:	Selective GABA_A-ρ antagonist
Chemical Name:	(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid
Purity:	≥98% (HPLC)
Molecular Weight:	161.14

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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
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	182485-36-5
PubChem ID	5520
InChi Key	MFUKVPOVVKKLRQ-UHFFFAOYSA-N
Smiles	OP(C1=CCNCC1)(C)=O

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water		100

Preparing Stock Solutions

The following data is based on the product molecular weight 161.14.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	6.21 mL	31.03 mL	62.06 mL
5 mM	1.24 mL	6.21 mL	12.41 mL
10 mM	0.62 mL	3.10 mL	6.21 mL
50 mM	0.12 mL	0.62 mL	1.24 mL

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References

References are publications that support the biological activity of the product.

Xu The involvement of GABA-C receptors in paired pulse depression of inhibitory postsynaptic currents in rat hippocampal CA1 pyramidal neurons. Exp.Neurol. 2009 PMID: 19100735
Chebib GABA_C receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes. Eur.J.Pharmacol. 1998 PMID: 9797041
Ragozzino Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist. Mol.Pharmacol. 1996 PMID: 8863850
Murata The first selective antagonist for a GABA_c receptor. Bioorg.Med.Chem.Lett.

Citations for TPMPA (12)

Showing 1 - 10 of 12 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for TPMPA include:

Hellmer et al. (2018) A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina. Physiol Rep. 6:e13885
PMID: 30338673
Manookin et al. (2018) Neural Mechanisms Mediating Motion Sensitivity in Parasol Ganglion Cells of the Primate Retina. Neuron. 97:1327
PMID: 29503188
Chaffiol et al. (2017) DA Regulation of GABAA Receptors Contributes to Light/Dark Modulation of the ON-Cone Bipolar Cell Receptive Field Surround in the Retina. Curr Biol. 27:2600
PMID: 28844643
Elgueta et al. (2015) Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells. J Neurosci. 9:6
PMID: 25709566
Murphy-Baum and Taylor (2015) The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina. Vis Neurosci. 35:13336
PMID: 26424882
Antonelli et al. (2014) Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction. Nat Commun. 5:5066
PMID: 25297980
Vielma et al. (2014) Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells. PLoS One. 9:e114330
PMID: 25463389
Jensen (2013) Effects of a metabotropic glutamate 1 receptor antagonist on light responses of retinal ganglion cells in a rat model of retinitis pigmentosa. PLoS One. 8:e79126
PMID: 24205371
Lindstrom et al. (2010) Retinal input to efferent target amacrine cells in the avian retina. J Neurosci. 27:103
PMID: 20650017
Olmos-Serrano et al. (2010) Defective GABAergic neurotransmission and pharmacological rescue of neuronal hyperexcitability in the amygdala in a mouse model of fragile X syndrome. Br J Pharmacol. 30:9929
PMID: 20660275
Gascon et al. (2006) GABA regulates dendritic growth by stabilizing lamellipodia in newly generated interneurons of the olfactory bulb. J Neurosci. 26:12956
PMID: 17167085
Wood et al. (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Front Cell Neurosci. 131:1050
PMID: 11082110

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Used in inhibitor cocktail

Name: Anonymous

Species: Rat

Assay Type: In Vitro

Cell Line/Tissue: Retinal rod bipolar cells

Retinal dissections were performed in HEPES-buffered extracellular solution containing inhibitor cocktail50 umol/L

PMID: 30338673

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