GS 39783

Name: GS 39783
Brand: Tocris Bioscience
SKU: 2001

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

Citations (352)

COA / SDS

Positive allosteric modulator of GABAB receptors

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Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Positive allosteric modulator of GABAB receptors

View all GABA-B Receptor Modulators »

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

Molecular Weight

337.44

Formula

C₁₅H₂₃N₅O₂S

Storage

Store at RT

Purity

≥98% (HPLC)

Chemical Name

N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine

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.

Solubility

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

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.

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

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Background References

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