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Submit ReviewCGP 7930
Description: Positive allosteric modulator of GABAB receptors
Chemical Name: 3,5-bis(1,1-Dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
Purity: ≥98% (HPLC)
Biological Activity for CGP 7930
CGP 7930 is a positive allosteric modulator of GABAA and GABAB receptors. Increases the potency and efficacy of GABA at both recombinant and native GABAB 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 GABAA 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 GABAA receptor currents by specific type-A receptor agonist Muscimol (EC50 = 2.0 μM). CGP7930 potentiates GABAA 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 GABAA receptor signaling in HEK 293 cells. CGP 7930 reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration.
Compound Libraries for CGP 7930
CGP 7930 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CGP 7930
| M. Wt | 292.46 |
| Formula | C19H32O2 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 57717-80-3 |
| PubChem ID | 5024764 |
| InChI Key | XLWJPQQFJNGUPA-UHFFFAOYSA-N |
| Smiles | CC(C)(CO)CC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C |
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.
Solubility Data for CGP 7930
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 29.25 | 100 | |
| DMSO | 29.25 | 100 |
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 will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.42 mL | 17.1 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 |
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Product Datasheets for CGP 7930
References for CGP 7930
References are publications that support the biological activity of the product.
Chen et al (2006) Differential modulation by the GABAB 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. 317 1170 PMID: 16507713
Liang et al (2006) The GABAB receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 50 632 PMID: 16406445
Urwyler et al (2001) Positive allosteric modulation of native and recombinant γ-aminobutyric acidB receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol.Pharmacol. 60 963 PMID: 11641424
Hannan et al (2023) CGP7930 - An allosteric modulator of GABABRs, GABAARs and inwardly-rectifying potassium channels. Neuropharmacology 238 109644 PMID: 37422181
If you know of a relevant reference for CGP 7930, please let us know.
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Keywords: CGP 7930, CGP 7930 supplier, Positive, modulators, GABAB, receptors, GABAA, receptor, PAM, CGP7930, GIRK, Inward, Rectifier, Potassium, Channels, Kir, Receptors, rectifier, 1513, Tocris Bioscience
3 Citations for CGP 7930
Citations are publications that use Tocris products. Selected citations for CGP 7930 include:
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. PLoS One 5 10468 PMID: 26020477
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540
Rondard et al (2008) Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning. EMBO J 27 1321 PMID: 18388862
Do you know of a great paper that uses CGP 7930 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.