TPMPA

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Cat.No. 1040 - TPMPA | C6H12NO2P | CAS No. 182485-36-5
Description: Selective GABAA-ρ antagonist
Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble 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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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

Murata et al (1996) The first selective antagonist for a GABAc receptor. Bioorg.Med.Chem.Lett. 6 2073 PMID:


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Keywords: TPMPA, supplier, Selective, GABAC, antagonists, Receptors, GABAA-rho, Receptors, Tocris Bioscience

6 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

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

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


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Literature in this Area

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Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

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GABA Receptors

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.

Pathways for TPMPA

Protocols

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