CGP 7930

Biological Activity

CGP 7930 is a positive allosteric modulator of GABA_A and GABA_B receptors. Increases the potency and efficacy of GABA at both recombinant and native GABA_B receptors (EC₅₀ values are 4.60 μM and 5.37 μM respectively) and enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. In HEK-293 cells expressing recombinant GABA_A receptor, CGP 7930 increases the potency and efficacy of GABA (EC₅₀ values are 1.0 μM and 1.7 μM at α4β3δ and α1β2γ2L receptors respectively). In cultured hippocampal neurons, pre-application of CGP 7930 causes concentration-dependent potentiation of GABA_A receptor currents by specific type-A receptor agonist Muscimol (EC₅₀ = 2.0 μM). CGP7930 potentiates GABA_A receptor-mediated tonic inhibition, reduces the frequency of inhibitory postsynaptic currents and prolongs rise and decay times. CGP 7930 also blocks G protein-coupled inwardly rectifying K+ (GIRK) channels diminishing GABA_A receptor signaling in HEK 293 cells. CGP 7930 reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Differential modulation by the GABA_B receptor allosteric potentiator 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)-phenol (CGP7930) of synaptic transmission in the rat hippocampal CA1 area.
   Chen et al.
   J.Pharmacol.Exp.Ther., 2006;317:1170
2. The GABA_B receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats.
   Liang et al.
   Neuropharmacology, 2006;50:632
3. Positive allosteric modulation of native and recombinant γ-aminobutyric acid_B receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501.
   Urwyler et al.
   Mol.Pharmacol., 2001;60:963

Product Datasheets