CGP 7930

Product Description

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.

Solubility

Preparing Stock Solutions for CGP 7930

The following data is based on the product molecular weight 292.46

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.42 mL	17.10 mL	34.19 mL
5 mM	0.68 mL	3.42 mL	6.84 mL
10 mM	0.34 mL	1.71 mL	3.42 mL
50 mM	0.07 mL	0.34 mL	0.68 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Hannan CGP7930 - An allosteric modulator of GABA_BRs, GABA_ARs and inwardly-rectifying potassium channels. Neuropharmacology 2023 PMID: 37422181
• Liang The GABA_B receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 2006 PMID: 16406445
• Urwyler 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. Mol.Pharmacol. 2001 PMID: 11641424
• Chen 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. J.Pharmacol.Exp.Ther. 2006 PMID: 16507713