GS 39783

Name: GS 39783
Brand: Tocris Bioscience
SKU: 2001

Tocris Bioscience, part of Bio-Techne | Catalog # 2001

Citations (353)

COA / SDS

Positive allosteric modulator of GABAB receptors

Key Product Details

Description:	Positive allosteric modulator of GABA_B receptors
Chemical Name:	N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
Purity:	≥98% (HPLC)
Molecular Weight:	337.44

View Full Technical Details for GS 39783

Technical Data
Citations

Biological Activity for GS 39783

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.

Technical Data for GS 39783

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GS 39783

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

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for GS 39783

References are publications that support the biological activity of the 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