GS 39783

Key Product Details

Product Description

GS 39783 is a positive allosteric modulator of GABA_B receptor function. Potentiates the effects of GABA on [³⁵S]GTPγS binding at recombinant and native GABA_B 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.

Product Specifications for GS 39783

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

Solubility

Preparing Stock Solutions for GS 39783

The following data is based on the product molecular weight 337.44.

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
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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 356 publications citing the usage of this product.

• Pizzo Elucidation of the neural circuits activated by a GABA_B receptor positive modulator: Relevance to anxiety. Neuropharmacology 2018 PMID: 28734870
• Cryan 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. 2004 PMID: 15113848
• Mombereau GABA_B 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. 2007 PMID: 17215447
• Urwyler N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of γ-aminobutyric acid_B receptor function. J.Pharmacol.Exp.Ther. 2003 PMID: 12954816

Product Documents for GS 39783