Cat. No. 1040
Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)met
Biological ActivityA 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.
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.
Certificate of Analysis / Safety Data Sheet
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.
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.
Murata et al (1996) The first selective antagonist for a GABAc receptor. Bioorg.Med.Chem.Lett. 6 2073.
Ragozzino et al (1996) Design and in vitro pharmacology of a selective γ-aminobutyric acidc receptor antagonist. Mol.Pharmacol. 50 1024. PMID: 8863850.
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Citations are publications that use Tocris products. Selected citations for TPMPA include:
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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Keywords: TPMPA, supplier, Selective, GABAC, antagonists, Receptors, Tocris Bioscience, GABAA-ρ Receptor Antagonist products
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