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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowGABAA and GABAC ReceptorsarrowGABAC ReceptorsarrowAntagonists
Cat.No. Product Name
1040 TPMPA
Price and Availability

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TPMPA

Other Information:

Not for sale in the USA
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 r1 receptors over r2 receptors.

Technical Data:

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M.Wt: 161.14
Formula: C6H12NO2P
Storage: Store at RT
Solubility: Soluble to 100 mM in Water
CAS No: [182485-36-5]

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    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. Chebib et al (1998) GABAC receptor antagonists differentiate between human r1 and r2 receptors expressed in Xenopus oocytes. Eur.J.Pharmacol. 357 227.
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    Keywords: TPMPA, Ligand-gated Ion Channels, Selective GABAC Antagonist, Tocris Bioscience
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