TPMPACat. No. 1040 |
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Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid |
Biological Activity
A selective, competitive GABAC 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.Certificate of Analysis / Safety Data Sheet
References
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.
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.
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.
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Keywords: TPMPA, supplier, Selective, GABAC, antagonists, Receptors
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