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 / Product Datasheet / 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:
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.
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.
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Keywords: TPMPA, supplier, Selective, GABAC, antagonists, Receptors, Tocris Bioscience, GABAA-ρ Receptor Antagonist products
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