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Biological Activity for TPMPA
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 for TPMPA
|Storage||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.
Solubility Data for TPMPA
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TPMPA
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||3.1 mL||6.21 mL|
|50 mM||0.12 mL||0.62 mL||1.24 mL|
References for TPMPA
References are publications that support the biological activity of the product.
Chebib et al (1998) GABAC receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes. Eur.J.Pharmacol. 357 227 PMID: 9797041
Ragozzino et al (1996) Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist. Mol.Pharmacol. 50 1024 PMID: 8863850
Xu et al (2009) The involvement of GABA-C receptors in paired pulse depression of inhibitory postsynaptic currents in rat hippocampal CA1 pyramidal neurons. Exp.Neurol. 216 243 PMID: 19100735
Murata et al (1996) The first selective antagonist for a GABAc receptor. Bioorg.Med.Chem.Lett. 6 2073
If you know of a relevant reference for TPMPA, please let us know.
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Keywords: TPMPA, TPMPA supplier, Selective, GABAC, antagonists, Receptors, GABAA-rho, GABAA-ρ, GABA-A, 1040, Tocris Bioscience
12 Citations for TPMPA
Citations are publications that use Tocris products. Selected citations for TPMPA include:
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
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
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
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
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
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
Antonelli et al (2014) Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction. Nat Commun 5 5066 PMID: 25297980
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
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
Do you know of a great paper that uses TPMPA from Tocris? Please let us know.
Reviews for TPMPA
Average Rating: 5 (Based on 1 Review.)
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Retinal dissections were performed in HEPES-buffered extracellular solution containing inhibitor cocktail50 umol/L
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.