GS 39783

Catalog #: 2001
2 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
2001/10
2001/50

GS 39783 | CAS No. 39069-52-8 | GABA-B Receptor Modulators

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Description: Positive allosteric modulator of GABAB receptors

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

Purity: ≥98%

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Product Details

Citations (2)

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Biological Activity

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

M.Wt:

337.44

Formula:

C₁₅H₂₃N₅O₂S

Solubility:

Soluble to 5 mM in ethanol and to 10 mM in DMSO

Purity:

≥98%

Storage:

Store at RT

CAS No:

39069-52-8

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.

Background References

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.
Urwyler et al.
J.Pharmacol.Exp.Ther., 2003;307:322
GABA_B receptor-positive modulation-induced blockade of the rewarding effects of nicotine is associated with a reduction in nucleus accumbens ΔFosB accumulation.
Mombereau et al.
J.Pharmacol.Exp.Ther., 2007;321:172
Elucidation of the neural circuits activated by a GABA_B receptor positive modulator: Relevance to anxiety.
Pizzo et al.
Neuropharmacology, 2018;136:129
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
Cryan et al.
J.Pharmacol.Exp.Ther., 2004;310:952

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Citations for GS 39783

The citations listed below are publications that use Tocris products. Selected citations for GS 39783 include:

2 Citations: Showing 1 - 2

GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
Authors: Zhang Et al.
Sci Rep 2015;5:10468
Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome.
Authors: Pacey Et al.
Sci Rep 2011;338:897

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