Cat. No. 2001
Chemical Name: N,N'-Dicyclopentyl-2-(methylthio)-5-
Biological ActivityPositive 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.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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.
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 benzodiazepines. J.Pharmacol.Exp.Ther. 310 952. PMID: 15113848.
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.
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Citations are publications that use Tocris products. Selected citations for GS 39783 include:
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Sci Rep 5 10468. PMID: 26020477.
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.
Do you know of a great paper that uses GS 39783 from Tocris? If so please let us know.
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Keywords: GS 39783, supplier, Positive, modulators, GABAB, receptors, GS39783, Tocris Bioscience, GABAB Receptor Modulator products
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