Biological descriptionNovel, GABAB positive allosteric modulator (EC50 = 3 μM for [35S]GTPγS binding). Shows anxiolytic and antiaddictive effects in vivo. Blood-brain barrier permeable. Orally active.
Storage instructionsStore at -20°C. Store at -20°C long term. Store In the Dark. Store under Desiccating conditions. This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes.
Solubility overviewSoluble in DMSO to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Mombereau C et al. GABAB receptor-positive modulation-induced blockade of the rewarding properties of nicotine is associated with a reduction in nucleus accumbens DeltaFosB accumulation. J Pharmacol Exp Ther321:172-7 (2007).
Read more (PubMed: 17215447) »
Cryan JF et al. 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 Ther310:952-63 (2004).
Read more (PubMed: 15113848) »
Urwyler S et al. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J Pharmacol Exp Ther307:322-30 (2003).
Read more (PubMed: 12954816) »