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GS 39783

Cat. No. 2001

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

Biological Activity

Novel 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.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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 acid_B receptor function. J.Pharmacol.Exp.Ther. 307 322. PMID: 12954816.

Cryan et al (2004) Behavioral characterization of the novel GABA_B 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.

Mombereau et al (2007) 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. 321 172. PMID: 17215447.

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