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.
|Storage||Store at RT|
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.
|Solubility||Soluble to 100 mM in water|
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 solvent 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 are publications that support the products' biological activity.
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
If you know of a relevant reference for TPMPA, please let us know.
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Keywords: TPMPA, supplier, Selective, GABAC, antagonists, Receptors, GABAA-rho, Receptors, GABAA-rho, Receptors, Tocris Bioscience
6 Citations for TPMPA
Citations are publications that use Tocris products. Selected citations for TPMPA include:
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
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
Antonelli et al (2014) Pin1-dependent signalling negatively affects GABAergic transmission by modulating neuroligin2/gephyrin interaction. Nat Commun 5 5066 PMID: 25297980
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
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
Do you know of a great paper that uses TPMPA from Tocris? If so please let us know.
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Literature in this Area
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.