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Submit ReviewGS 39783
说明： Positive allosteric modulator of GABAB receptors
化学名： N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
纯度： ≥98% (HPLC)
生物活性 for GS 39783
GS 39783 is a positive allosteric modulator of GABAB receptor function. Potentiates the effects of GABA on [35S]GTPγS binding at recombinant and native GABAB receptors (EC50 values are 2.1 and 3.1μM respectively). Decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines.
技术数据 for GS 39783
| 分子量 | 337.44 |
| 公式 | C15H23N5O2S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 39069-52-8 |
| PubChem ID | 6604928 |
| InChI Key | GSGVDKOCBKBMGG-UHFFFAOYSA-N |
| Smiles | CSC1=NC(NC2CCCC2)=C(C(NC2CCCC2)=N1)[N+]([O-])=O |
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 GS 39783
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 1.69 | 5 | |
| DMSO | 3.37 | 10 |
制备储备液 for GS 39783
以下数据基于产品分子量 337.44。 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 |
|---|---|---|---|
| 0.1 mM | 29.63 mL | 148.17 mL | 296.35 mL |
| 0.5 mM | 5.93 mL | 29.63 mL | 59.27 mL |
| 1 mM | 2.96 mL | 14.82 mL | 29.63 mL |
| 5 mM | 0.59 mL | 2.96 mL | 5.93 mL |
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产品说明书 for GS 39783
参考文献 for GS 39783
参考文献是支持产品生物活性的出版物。
Urwyler et al (2003) N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of γ-aminobutyric acidB receptor function. J.Pharmacol.Exp.Ther. 307 322 PMID: 12954816
Cryan et al (2004) Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: anxiolytic-like activity without side effects associated with bac. or benzo J.Pharmacol.Exp.Ther. 310 952 PMID: 15113848
Mombereau et al (2007) GABAB receptor-positive modulation-induced blockade of the rewarding effects of nicotine is associated with a reduction in nucleus accumbens ΔFosB accumulation. J.Pharmacol.Exp.Ther. 321 172 PMID: 17215447
Pizzo et al (2018) Elucidation of the neural circuits activated by a GABAB receptor positive modulator: Relevance to anxiety. Neuropharmacology 136 129 PMID: 28734870
If you know of a relevant reference for GS 39783, please let us know.
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关键词: GS 39783, GS 39783 supplier, Positive, modulators, GABAB, receptors, GS39783, PAM, Receptors, 2001, Tocris Bioscience
2 篇 GS 39783 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GS 39783 的部分引用包括：
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Sci Rep 5 10468 PMID: 26020477
Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Sci Rep 338 897 PMID: 21636656
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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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