Catalog Number: 2001
Chemical Name: N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
Biological Activity
Positive 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.
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. All Tocris products are intended for laboratory research use only.
Background References
  1. 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.
    Urwyler et al.
    J.Pharmacol.Exp.Ther., 2003;307:322
  2. 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 benzo
    Cryan et al.
    J.Pharmacol.Exp.Ther., 2004;310:952
  3. GABAB 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
Citations:

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

2 Citations: Showing 1 - 2
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  1. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Sci Rep 2015;5:10468
  2. 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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