GS 39783

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Cat.No. 2001 - GS 39783 | C15H23N5O2S | CAS No. 39069-52-8
Description: Positive modulator at GABAB receptors
Chemical Name: N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

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.

Technical Data

M. Wt 337.44
Formula C15H23N5O2S
Storage Store at RT
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.37 10
ethanol 1.69 5

Preparing Stock Solutions

The following data is based on the product molecular weight 337.44. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.96 mL 14.82 mL 29.63 mL
5 mM 0.59 mL 2.96 mL 5.93 mL
10 mM 0.3 mL 1.48 mL 2.96 mL
50 mM 0.06 mL 0.3 mL 0.59 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 baclofen 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


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Keywords: GS 39783, supplier, Positive, modulators, GABAB, receptors, GS39783, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience

2 Citations for GS 39783

Citations are publications that use Tocris products. Selected citations for GS 39783 include:

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

Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Sci Rep 5 10468 PMID: 26020477


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