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Submit ReviewCGP 7930
说明： Positive allosteric modulator of GABAB receptors
化学名： 3,5-bis(1,1-Dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for CGP 7930
CGP 7930 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for CGP 7930
| 分子量 | 292.46 |
| 公式 | C19H32O2 |
| 储存 | Desiccate at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CGP 7930
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 29.25 | 100 | |
| DMSO | 29.25 | 100 |
制备储备液 for CGP 7930
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for CGP 7930
参考文献 for CGP 7930
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 CGP 7930 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CGP 7930 的部分引用包括：
Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. PLoS One 5 10468 PMID: 26020477
Rondard et al (2008) Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning. EMBO J 27 1321 PMID: 18388862
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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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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