Tocris/TPMPA/1040/10/10 mg

Biological Activity

A selective, competitive GABA_A-ρ antagonist with only minimal effects on GABA_A and GABA_B receptors (K_b 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

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

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.

Product Datasheets

References

References are publications that support the products' biological activity.

Chebib et al (1998) GABA_C 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 GABA_c receptor. Bioorg.Med.Chem.Lett. 6 2073 PMID: